I-Paclitaxel (Taxol) CAS 33069-62-4 Assay (HPLC) 97.0~102.0%
I-Shanghai Ruifu Chemical Co., Ltd. ngumenzi ohamba phambili wePaclitaxel (Taxol) (CAS: 33069-62-4) enomgangatho ophezulu.I-Ruifu Chemical inokubonelela ngenkonzo yehlabathi jikelele, ixabiso elikhuphisanayo, inkonzo egqwesileyo, encinci kunye nezixa ezininzi ezikhoyo.Thenga iPaclitaxel (Taxol),Please contact: alvin@ruifuchem.com
| Igama leMchiza | Paclitaxel |
| Izithethantonye | Taxol;Abraxane;iGenaxol;iGenetaxyl;I-OncoGel;Pacliex;(-)-Paclitaxel |
| Ubume beStokhwe | Kwi-Stock, iMveliso yoRhwebo |
| Inombolo yeCAS | 33069-62-4 |
| Ifomula yeemolekyuli | C47H51NO14 |
| Ubunzima beMolekyuli | 853.92 g/mol |
| Indawo yokunyibilika | 211℃(Disemba) |
| Ukuxinana | 0.200 |
| Ukunyibilika kwamanzi | Ayinyibilikiyo emanzini |
| Ukunyibilika | Inyibilika ngokulula kwiChloroform, iAcetone kunye nezinye izinyibilikisi zeOrganic. |
| Uzinzo | Izinzile.Ayihambelani neeAgents eziOxidizing ezinamandla.Ukutsha. |
| I-COA kunye ne-MSDS | Iyafumaneka |
| Isampulu | Iyafumaneka |
| Imvelaphi | Shanghai, China |
| Uphawu | Ruifu Chemical |
| Izinto | Iinkcukacha | Iziphumo |
| Imbonakalo | Umgubo weCrystalline oMhlophe, ongenavumba | Iyahambelana |
| Isazisi (A) | I-IR: Ingqinelana ne-RS | Iyahambelana |
| Ukuchongwa (B) | I-HPLC: I-RT Concordant kunye ne-RS | Iyahambelana |
| Ukujikeleziswa okuthe ngqo | -49.0 ° ukuya -55.0 ° | -52.3 ° |
| Amanzi nguKarl Fischer | ≤4.00% | 0.91% |
| Intsalela kwi-Ignition | ≤0.20% | 0.02% |
| Iintsimbi ezinzima (Pb) | ≤20ppm | <20ppm |
| IiCompounds eziyeleleneyo | ||
| Iyonke | ≤2.00% | 0.11% |
| I-10-Deacetylbaccatin III | ≤0.10% | Ayifunyanwa |
| Baccatin III | ≤0.20% | Ayifunyanwa |
| Ifotodegradant | ≤0.10% | Ayifunyanwa |
| 10-Deacetylpaclitaxel | ≤0.50% | 0.04% |
| 2-Debenzoylpaclitaxel-2-Pentenoate | ≤0.70% | Ayifunyanwa |
| 7-Epipaclitaxel | ≤0.40% | 0.014% |
| 10,13-Bissidechainpaclitaxel | ≤0.50% | 0.022% |
| 7-Acetylpaclitaxel | ≤0.60% | Ayifunyanwa |
| I-13-Tes-baccatin III | ≤0.10% | 0.004% |
| 7-Tes-Paclitaxel | ≤0.30% | Ayifunyanwa |
| Okunye Ukungcola Komntu Ngamnye | ≤0.10% | Iyahambelana |
| 0ubumdaka obuguquguqukayo | Iyahambelana | |
| Hexan | ≤290ppm | 31ppm |
| IAceton | ≤5000ppm | 1210ppm |
| Uvavanyo (HPLC) | 97.0 ~ 102.0% (ibalwe kwi-anhydrous, isiseko se-solvent-free) | 99.88% |
| Iimvavanyo zoMda weMicrobial | ||
| Ubalo olupheleleyo lweAerobic Microbial | ≤100 cfu/g | <100 cfu/g |
| Staphylococcus Aureus | Ukungabikho | Ukungabikho |
| Salmonella | Ukungabikho | Ukungabikho |
| Escherichia Coli | Ukungabikho | Ukungabikho |
| Iintsholongwane ze-Endotoxins | ≤0.4EU/mg | <0.4EU/mg |
| Ukuqukumbela | Imveliso ivavanyiwe kwaye ihambelana ne-USP43 Paclitaxel | |
Umqulu:Ibhotile eFluorinated, iAluminium foil bag, 25kg/Cardboard Drum, okanye ngokwemfuno yomthengi.
Imeko yoGcino:Gcina isikhongozeli sivalwe ngokuqinileyo kwaye usigcine kwindawo epholileyo, eyomileyo (2~8℃) kunye nendawo yokugcina impahla engena moya ikude kwizinto ezingahambelaniyo.Khusela ukukhanya kunye nokufuma.
Ukuhambisa ngenqanawe:Zisa kwihlabathi liphela ngomoya, ngeFedEx / DHL Express.Ukubonelela ngokukhawuleza nangokuthembekileyo.
Paclitaxel
C47H51NO14 853.91
Benzenepropanoic acid, -(benzoylamino) -hydroxy-, 6,12b-bis(acetyloxy) -12-(benzoyloxy) -2a,3,4,4a,5,6,9,10,11,12,12a,12b -dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl ester, [2aR-[2a,4,4a,6,9(R*,S*),11,12,12a,12b]]-.
(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-1,2a,3,4,4a,6,9,10,11,12,12a,12b-Dodecahydro-4,6, 9,11,12,12b-hexahydroxy-4a,8,13,13-tetramethyl-7,11-methano-5H-cyclodeca[3,4]-benz[1,2-b]oxet-5-enye 6, I-12b-diacetate, i-12-benzoate, i-9-ester kunye (2R, 3S)-N-benzoyl-3-phenylisoserine [33069-62-4].
I-Paclitaxel iqulethe ngaphantsi kweepesenti ze-97.0 kwaye ingekho ngaphezu kweepesenti ze-102.0 ze-C47H51NO14, ezibalwe kwi-anhydrous, i-solvent-free basis.
[Isilumkiso-I-Paclitaxel yi-cytotoxic.Ukhathalelo olukhulu kufuneka luthathwe ukunqanda ukuphefumla amasuntswana ePaclitaxel kwaye uveze ulusu kuwo.]
Ukupakishwa nokugcinwa-Londoloza kwizikhongozeli eziqinileyo, ezikwaziyo ukumelana nokukhanya, kwaye ugcine ubushushu begumbi elilawulwayo.
Ukuleyibhile-Ukuleyibhile kubonisa uhlobo lwenkqubo esetyenziselwa ukuvelisa izinto kunye novavanyo lweekhompawundi eziNxulumeneyo ezihambelanayo nazo.
Imigangatho yezalathiso ye-USP <11>-
USP Endotoxin RS
USP Paclitaxel RS Cofa ukujonga iSakhiwo
USP Paclitaxel Related Compound A RS
Cephalomannine.
USP Paclitaxel Related Compound B RS
10-Deacetyl-7-Epipaclitaxel.
USP Paclitaxel Umxube wokungcola RS
Umxube wePaclitaxel kunye nezi zixhobo zilandelayo ezihambelanayo: i-propyl analog, i-cephalomannine, i-sec-butyl analog, i-n-butyl analog, i-benzyl analog, i-baccatin VI, i-pentyl analog, kunye ne-7-epipaclitaxel.
Isazisi-
A: I-Infrared Absorption <197K>.
B: Ixesha lokugcinwa kwencopho enkulu kwichromatogram yoLungiselelo lwe-Assay ihambelana naleyo kwichromatogram yoLungiselelo oluMgangatho, njengoko lufunyenwe kwi-Assay.
Ukujikeleza okuthe ngqo kwe-781S: phakathi kwe-49.0 kunye ne-55.0 kwi-20, ibalwa kwisiseko se-anhydrous, i-solvent-free.
Isisombululo sovavanyo: 10 mg nge-mL, kwi-methanol.
Iimvavanyo ze-Microbial enumeration <61> kunye noVavanyo lwee-microorganisms ezichaziweyo <62>-Itotali ye-aerobic microbial count ayidluli kwi-100 cfu ngeg.Ihlangabezana neemfuno zeemvavanyo zokungabikho kwe-Staphylococcus aureus, i-Pseudomonas aeruginosa, iintlobo ze-Salmonella, kunye ne-Escherichia coli.
I-Bacterial endotoxins 85-Ayiqukethe ngaphezu kwe-0.4 USP Endotoxin Unit nge-mg ye-paclitaxel.
Amanzi, Indlela Ic <921>: hayi ngaphezulu kwe-4.0%.
Intsalela ekutshiseni <281>: hayi ngaphezulu kwe-0.2%.
Iintsimbi ezinzima, Indlela II <231>: 0.002%.
Izikhonkwane eziyeleleneyo-
uvavanyo 1 (kwizinto ezibhalwe njengezodwa kwimithombo yendalo)-Ukuba izinto ziyahambelana nolu vavanyo, ukuleyibhile kubonisa ukuba idibana ne-USP eNxulumene neekhompawundi Test 1.
Diluent-Lungiselela njengoko kuyalelwe kwi-Assay.
Isisombululo A-Lungisa i-acetonitrile ehluziweyo kunye ne-degassed.
Isisombululo B-Lungisa amanzi ahluziweyo kunye negassed.
Isigaba esiphathwayo-Sebenzisa imixube eguquguqukayo yeSisombululo A kunye neSisombululo B njengoko kumiselwe inkqubo yeChromatographic.Yenza uhlengahlengiso xa kukho imfuneko (jonga ukufaneleka kweNkqubo phantsi kweChromatography 621).
Isisombululo sokufaneleka kwenkqubo-Dibanisa ngokuchanekileyo ubungakanani be-USP Paclitaxel Related Compound A RS kunye ne-USP Paclitaxel Related Compound B RS kwi-methanol ukufumana isisombululo esinoxinzelelo olwaziwayo malunga ne-10 µg nganye ngemL nganye.Dlulisa i-5.0 mL yesi sisombululo kwi-flask ye-volumetric ye-50-mL, yihlambulule nge-Diluent ukuya kwivolumu, kwaye udibanise.
Isisombululo esisemgangathweni-Dibanisa, ngoncedo lwe-sonication, ubungakanani obulinganiswe ngokuchanekileyo be-USP Paclitaxel RS kwi-Diluent, kunye nokunciphisa ubuninzi, kunye ne-stepwise ukuba kuyimfuneko, kunye ne-Diluent ukufumana isisombululo esinoxinzelelo olwaziwayo malunga ne-5 µg nge-mL.
Isisombululo sovavanyo-Sebenzisa ukulungiswa koVavanyo.
Inkqubo yeChromatographic (bona iChromatography <621>) -I-chromatograph yolwelo ixhotyiswe nge-227-nm detector kunye ne-4.6-mm × 25-cm ikholamu equlethe i-5-µm yokupakisha i-L43.Izinga lokuhamba malunga ne-2.6 mL ngomzuzu.Ubushushu bekholomu bugcinwa kwi-30. I-chromatograph ihlelwe ngolu hlobo lulandelayo.
Ixesha (imizuzu) Isisombululo A (%) Isisombululo B (%) Uvavanyo
0–35 35 65 isokhrasi
35–60 35®80 65®20 umda womda
60–70 80®35 20®65 umyinge womda
70-80 35 65 isocraticChromatograph isisombululo sokufaneleka kweSistim, kwaye urekhode iimpendulo eziphezulu njengoko zichazwe kwiNkqubo: amaxesha okugcinwa okuhambelanayo malunga ne-0.78 ye-paclitaxel enxulumene nekhompawundi A kunye ne-0.86 ye-paclitaxel enxulumene ne-compound B (ngokunxulumene nexesha lokugcinwa kwe-paclitaxel efunyenwe kwi-paclitaxel isisombululo soVavanyo);kunye nesisombululo, R, phakathi kwe-paclitaxel enxulumene nekhompawundi A kunye ne-paclitaxel enxulumene nekhompawundi B ayikho ngaphantsi kwe-1.0.I-Chromatograph isisombululo soMgangatho, kwaye urekhode iimpendulo eziphakamileyo njengoko ziqondiswe kwiNkqubo: ukutenxa okusemgangathweni ohambelanayo kwiinaliti eziphindaphindayo akukho ngaphezu kwe-2.0%.
Inkqubo-Tofa umthamo (malunga ne-15 µL) yesisombululo soVavanyo kwichromatograph, urekhode ichromatogram, kwaye ulinganise iindawo zeencopho ezinkulu.Bala ipesenti yokungahlambuluki ngakunye kwinxalenye yePaclitaxel ethathwe yifomula:
100(NgoLwesihlanu / rU)
apho i-F iyinxalenye yempendulo ehambelanayo kwincopho nganye yokungcola (jonga iTheyibhile 1 ngexabiso);i-ri yindawo encopho yokungcola komntu ngamnye;kwaye i-ru yindawo ephezulu ye-paclitaxel.
Uluhlu loku-1
Ugcino Lwexesha Elinxulumeneyo Umba weMpendulo (F) Umda wegama (%)
0.24 1.29 Baccatin III 0.2
0.53 1.00 10-Deacetylpaclitaxel 0.5
0.57 1.00 7-Xylosylpaclitaxel 0.2
0.78 1.26 I-Cephalomannine (i-Paclitaxel ehambelana nekhompawundi A) a11
0.78 1.26 2'',3''-Dihydrocephalomanine a21
0.86 1.00 10-Deacetyl-7-epipaclitaxel (i-Paclitaxel enxulumene nekhompawundi B) 0.5
1.10 1.00 Benzyl analog3 b12
1.10 1.00 3'',4''-Dehydropaclitaxel C b22
1.40 1.00 7-Epicephalomanine 0.3
1.85 1.00 7-Epipaclitaxel 0.5
1 Isigqibo sisenokungaphelelanga kwezi ncopho, ngokuxhomekeke kwimilinganiselo ekhoyo;Isamba se-a1 kunye ne-a2 ayikho ngaphezu kwe-0.5%.
2 Isigqibo sisenokungaphelelanga kwezi ncopho, ngokuxhomekeke kwizixa-mali ezikhoyo;Isamba se-b1 kunye ne-b2 ayikho ngaphezu kwe-0.5%.
3 Igama lekhemikhali elilandelayo linikezelwe kwikhompawundi ehambelanayo, i-benzyl analog: Baccatin III 13-ester kunye (2R, 3S) -2-hydroxy-3-phenyl-3- (2-phenylacetylamino) propanoic acid.
Ukongeza kokungagqithisi kwimida yokungcola okunxulumene ne-paclitaxel kwiThebhile 1, akukho ngaphezu kwe-0.1% yobunye ukungcola okufunyenweyo;kwaye akukho ngaphezulu kwe-2.0% yokungcola okupheleleyo kufunyenwe.
uvavanyo 2 (ngezinto ezibhalwe njengoko ziveliswe inkqubo semisynthetic)— Ukuba izinto ziyahambelana nolu vavanyo, ileyibheli ibonisa ukuba idibana USP Related iikhompawundi Test 2.
Diluent-Sebenzisa i-acetonitrile.
Isisombululo A-Sebenzisa umxube ohluziweyo kunye ne-degassed yamanzi kunye ne-acetonitrile (3: 2).
Isisombululo B-Sebenzisa i-acetonitrile ehluziweyo kunye ne-degassed.
Isigaba esiphathwayo-Sebenzisa imixube eguquguqukayo yeSisombululo A kunye neSisombululo B njengoko kumiselwe inkqubo yeChromatographic.Yenza uhlengahlengiso xa kukho imfuneko (jonga ukufaneleka kweNkqubo phantsi kweChromatography 621).
Isisombululo sokufaneleka kwenkqubo-Dibanisa ngokuchanekileyo ubungakanani be-USP Paclitaxel RS kunye ne-USP Paclitaxel Related Compound B RS kwi-Diluent, shaking and sonicating xa kuyimfuneko, ukufumana isisombululo esinomlinganiselo owaziwayo malunga ne-0.96 mg kunye ne-0.008 mg nge-mL, ngokulandelanayo.
Isisombululo sovavanyo-Ukudlulisa malunga ne-10 mg ye-Paclitaxel, ilinganiswe ngokuchanekileyo, kwi-flask ye-volumetric ye-10-mL, chitha kwaye udibanise nge-Diluent ukuya kwivolumu, ukugubha kunye ne-sonicating xa kuyimfuneko, kwaye udibanise.
Inkqubo yeChromatographic (jonga i-Chromatography 621)— I-chromatograph yolwelo ixhotyiswe nge-227-nm detector kunye nekholamu ye-4.6-mm × 15-cm equlethe i-3-µm yokupakisha i-L1.Izinga lokuhamba malunga ne-1.2 mL ngomzuzu.Ubushushu bekholomu bugcinwa kwi-35. I-chromatograph ihlelwe ngolu hlobo lulandelayo.
Ixesha (imizuzu) Isisombululo A (%) Isisombululo B (%) Uvavanyo
0-20 100 0 isokhrasi
I-20-60 100®10 0®90 i-gradient yomgca
60-62 10®100 90®0 i-gradient yomgca
62-70 100 0 isocraticChromatograph isisombululo sokufaneleka kweSistim, kwaye urekhode iimpendulo eziphezulu njengoko ziqondiswe kwiNkqubo: amaxesha okugcinwa okuhambelanayo malunga ne-0.94 ye-paclitaxel ehambelana ne-compound B kunye ne-1.0 ye-paclitaxel;isisombululo, R, phakathi kwe-paclitaxel ehambelana ne-compound B kunye ne-paclitaxel ayikho ngaphantsi kwe-1.2;kunye nokutenxa komgangatho ozalanayo wokuphindaphinda iinaliti akukho ngaphezu kwe-2.0%.
Inkqubo-Ngokwahlukileyo tofa imithamo elinganayo (malunga ne-15 µL) yeDiluent kunye nesisombululo soVavanyo kwichromatograph, urekhode iichromatogram, kwaye ulinganise iindawo zazo zonke iincopho.Ukungahoyi naziphi na iincopho ngenxa yeDiluent.Bala ipesenti yokungahlambuluki ngakunye kwinxalenye yePaclitaxel ethathwe yifomula:
100(NgoLwesihlanu / rs)
apho i-F iyinxalenye yempendulo ehambelanayo yokungahlambuluki ngakunye (jonga iTheyibhile 2 ngexabiso);ri yindawo encopho yokungcola ngakunye okufunyenwe kwisisombululo soVavanyo;kwaye rs sisimbuku seendawo zazo zonke iincopho ezifunyenwe kwisisombululo soVavanyo.
Uluhlu lwesi-2
Ugcino Lwexesha Elinxulumeneyo Umba weMpendulo (F) Umda wegama (%)
0.11 1.24 10-Deacetylbaccatin III 0.1
0.20 1.29 Baccatin III 0.2
0.42 1.39 Ifotodegradant2 0.1
0.47 1.00 10-Deacetylpaclitaxel 0.5
0.80 1.00 2-Debenzoylpaclitaxel-2-pentenoate 0.7
0.921 1.00 Iringi ye-Oxetane ivuliwe, i-acetyl kunye ne-benzoyl yafuduka2 x1
0.921 1.00 10-Acetoacetylpaclitaxel x2
0.941 1.00 10-Deacetyl-7-epipaclitaxel (i-Paclitaxel enxulumene nekhompawundi B) x3
1.37 1.00 7-Epipaclitaxel 0.4
1.45 1.00 10,13-Bissidechainpaclitaxel2 0.5
1.54 1.00 7-Acetylpaclitaxel 0.6
1.80 1.75 13-Tes-baccatin III 0.1
2.14 1.00 7-Tes-paclitaxel 0.3
1 Isigqibo sisenokungaphelelanga kwezi ncopho, ngokuxhomekeke kwimilinganiselo ekhoyo;isixa-mali sika-x1, x2, kunye no-x3 asikho ngaphezu kwe-0.4%.
2 La magama ekhemikhali alandelayo abelwa kwiikhompawundi ezinxulumene nePhotodegradant;I-Oxetane ring yavulwa, i-acetyl kunye ne-benzoyl yafuduka;kunye ne-10,13-Bissidechainpaclitaxel:
Ifotodegradant
(1R,2R,4S,5S,7R,10S,11R,12S,13S,15S,16S)-2,10-diacetyloxy-5,13-dihydroxy-4,16,17,17-tetramethyl-8-oxa- 3-oxo-12-phenylcarbonyloxypentacyclo[11.3.1.01,11.04,11.07,10]heptadec-15-yl
(2R,3S)-2-hydroxy-3-phenyl-3-(phenylcarbonylamino)propanoate
I-Oxetane ring yavulwa, i-acetyl kunye ne-benzoyl zafuduka
(1S,2S,3R,4S,5S,7S,8S,10R,13S)-5,10-diacetyloxy-1,2,4,7-tetrahydroxy-8,12,15,15-tetramethyl-9-oxo- 4-(phenylcarbonyloxymethyl)tricyclo[9.3.1.03,8]pentadec-11-en-13-yl
(2R,3S)-2-hydroxy-3-phenyl-3-(phenylcarbonylamino)propanoate
10,13-Bissidechainpaclitaxel
Baccatin III 13-ester kunye (2R,3S) -2-hydroxy-3-phenyl-3- (phenylcarbonylamino) propanoic acid, 10-ester nge (2S,3S) -2-hydroxy-3-phenyl-3-(phenylcarbonylamino ipropanoic acid
Ukongeza kokungagqithisi kwimida yokungcola okunxulumene ne-paclitaxel kwiThebhile 2, akukho ngaphezu kwe-0.1% yayo nayiphi na enye into efunyenweyo;kwaye akukho ngaphezulu kwe-2.0% yokungcola okupheleleyo kufunyenwe.
uvavanyo 3 (kwizinto ezibhalwe njengoko ziveliswe inkqubo yeseli yesityalo fermentation)— Ukuba imathiriyeli ihambelana nolu vavanyo, ileyibhile ibonisa ukuba idibana ne-USP Related compounds Test 3.
Isisombululo A-Lungisa umxube ohluziweyo kunye ne-degassed yamanzi kunye ne-acetonitrile (3: 2).
Isisombululo B-Lungisa i-acetonitrile ehluziweyo kunye ne-degassed.
Isigaba esiphathwayo-Sebenzisa imixube eguquguqukayo yeSisombululo A kunye neSisombululo B njengoko kumiselwe inkqubo yeChromatographic.Yenza uhlengahlengiso xa kukho imfuneko (jonga ukufaneleka kweNkqubo phantsi kweChromatography 621).
Isisombululo sokufaneleka kwenkqubo-Dissolve USP Paclitaxel Impurity Mixture RS kwi-acetonitrile, i-sonicating xa kuyimfuneko, ukufumana isisombululo esinoxinzelelo olwaziwayo malunga ne-1 mg nge-mL.
Isisombululo esisemgangathweni-Dibanisa ubungakanani obulinganiswe ngokuchanekileyo be-USP Paclitaxel RS kwi-acetonitrile, i-sonicating xa kuyimfuneko, ukufumana isisombululo esinoxinzelelo olwaziwayo malunga ne-1 mg nge-mL.
Isisombululo sovavanyo-Ukudluliselwa malunga ne-10 mg ye-Paclitaxel, ilinganiswe ngokuchanekileyo, kwi-flask ye-volumetric ye-10-mL.Dlulisa kwaye uhlambulule nge-acetonitrile ukuya kwivolumu, i-sonicating xa kuyimfuneko, kwaye udibanise.
Inkqubo yeChromatographic (jonga i-Chromatography 621)— I-chromatograph yolwelo ixhotyiswe nge-227-nm detector kunye nekholamu ye-4.6-mm × 15-cm equlethe i-3-µm yokupakisha i-L1.Izinga lokuhamba malunga ne-1.2 mL ngomzuzu.Ichromatograph icwangciswe ngolu hlobo lulandelayo.
Ixesha (imizuzu) Isisombululo A (%) Isisombululo B (%) Uvavanyo
0-28 100 0 isokhrasi
28-33 100®98 0®2 i-gradient yomgca
33–58 98®10 2®90 umda womda
58-60 10 90 isokhrasi
60-63 10®100 90®0 i-gradient yomgca
63-70 100 0 isocraticChromatograph isisombululo sokufaneleka kweSistim, kwaye urekhode iimpendulo eziphakamileyo njengoko ziqondiswe kwiNkqubo: isisombululo, R, phakathi kwe-paclitaxel kunye ne-benzyl analog ayikho ngaphantsi kwe-1.8.I-Chromatograph isisombululo soMgangatho, kwaye urekhode iimpendulo eziphakamileyo njengoko ziqondiswe kwiNkqubo: ukutenxa okusemgangathweni ohambelanayo kwiinaliti eziphindaphindayo akukho ngaphezu kwe-2.0%.[Qaphela-Ngenjongo yokuchongwa kwencopho, uqikelelo lwamaxesha ogcino oluqikelelwayo lunikiwe kwiThebhile 3. Amaxesha okugcina anxulumeneyo athelekiswa ne-Paclitaxel.]
Itheyibhile 3
Igama lomda wogcino lwexesha (%)
Ipropyl analog1 0.54 0.2
I-Cephalomannine (i-Paclitaxel enxulumene nekhompawundi A) 0.76 0.5
sec-Butyl analog2 0.81 0.2
n-Butyl analog3 0.89 0.1
I-analog ye-Benzyl 1.10 0.4
I-Baccatin VI 1.23 0.2
Ianalog yePentyl4 1.31 0.2
7-Epipaclitaxel 1.51 0.4
1 Igama lekhemikhali elilandelayo linikezelwe kwikhompawundi enxulumene ne-analog ye-Propyl: i-Baccatin III 13-ester ene- (2R, 3S) -3-butanoylamino-2-hydroxy-3-phenylpropanoic acid.
2 Igama lekhemikhali elilandelayo linikezelwe kwi-compound sec-Butyl analog: Baccatin III 13-ester kunye (2R, 3S) -2-hydroxy-3- (2-methylbutanoylamino) -3-phenylpropanoic acid.
3 Igama lekhemikhali elilandelayo linikezelwe kwikhompawundi enxulumene ne-n-Butyl analog:Baccatin III 13-ester ene (2S,3S) -2-hydroxy-3-(pentanoylamino) -3-phenylpropanoic acid.
4 Igama lekhemikhali elilandelayo linikezelwe kwikhompawundi enxulumene ne-analog yePentyl: Baccatin III 13-ester ene (2R,3S) -3-(hexanoylamino) -2-hydroxy-3-phenylpropanoic acid.
Inkqubo-Tofa umthamo (malunga ne-12 µL) yesisombululo soVavanyo kwichromatograph, urekhode ichromatogram, kwaye ulinganise iindawo zazo zonke iincopho.Bala ipesenti yokungahlambuluki ngakunye kwinxalenye yePaclitaxel ethathwe yifomula:
I-100(ri / rU)
apho ri yimpendulo yokungahlambuluki komntu ngamnye;kwaye i-rU sisimbuku seendawo zazo zonke iincopho ezifunyenwe kwisisombululo soVavanyo.Ukongeza kokungagqithisi kwimida yokungcola okunxulumene ne-paclitaxel kwiThebhile 3, akukho ngaphezu kwe-0.1% yayo nayiphi na enye into efunyenweyo;kwaye akukho ngaphezulu kwe-2.0% yokungcola okupheleleyo kufunyenwe.
Isivavanyi-
I-Diluent-Lungisa umxube we-methanol kunye ne-acetic acid (200: 1).
Isigaba esiphathwayo-Lungisa umxube ohluziweyo kunye ne-degassed yamanzi kunye ne-acetonitrile (11: 9).Yenza uhlengahlengiso xa kukho imfuneko (jonga ukufaneleka kweNkqubo phantsi kweChromatography 621).
Ukulungiswa okusemgangathweni-Dibanisa, usebenzisa i-sonication ukuba kuyimfuneko, ubungakanani obulinganiswe ngokuchanekileyo be-USP Paclitaxel RS kwi-Diluent, kunye nokunciphisa umthamo, kunye ne-stepwise ukuba kuyimfuneko, kunye ne-Diluent ukufumana isisombululo esinoxinzelelo olwaziwayo malunga ne-1 mg nge-mL.
Ukulungiswa kwe-Assay-Transfer malunga ne-10 mg ye-Paclitaxel, ilinganiswe ngokuchanekileyo, kwi-flask ye-volumetric ye-10-mL.Ukunyibilika kwi-Diluent, usebenzisa i-sonication ukuba kuyimfuneko, nciphisa nge-Diluent ukuya kwivolumu, kwaye udibanise.
Inkqubo yeChromatographic (bona iChromatography <621>) -I-chromatograph yolwelo ixhotyiswe nge-227-nm detector kunye ne-4.6-mm × 25-cm ikholamu equlethe i-5-µm yokupakisha i-L43.Izinga lokuhamba malunga ne-1.5 mL ngomzuzu.I-Chromatograph Ukulungiswa koMgangatho, kwaye urekhode iimpendulo eziphakamileyo njengoko zichazwe kwiNkqubo: i-tailing factor iphakathi kwe-0.7 kunye ne-1.3;kunye nokutenxa komgangatho ozalanayo wokuphindaphinda iinaliti akukho ngaphezu kwe-1.5%.
Inkqubo-Ngokwahlukileyo tofa imithamo elinganayo (malunga ne-10 µL) yoLungiso oluMgangatho kunye nolungiselelo loVavanyo kwichromatograph, urekhode iichromatograms, kwaye ulinganise iindawo zeencopho ezinkulu.Bala ubuninzi, kwi-mg, ye-C47H51NO14 kwisahlulo se-Paclitaxel esithathwe ngefomula:
10C(rU / rS)
apho i-C igxininise, kwi-mg nge-mL, ye-USP Paclitaxel RS kulungiselelo olusemgangathweni;kunye ne-rU kunye ne-rS ziyincopho yeempendulo ze-paclitaxel ezifunyenwe kulungiselelo lwe-Assay kunye nokulungiswa koMgangatho, ngokulandelanayo.
Ukuthenga njani?Nceda uqhagamshelaneDr. Alvin Huang: sales@ruifuchem.com or alvin@ruifuchem.com
Amava Eminyaka Eli-15?Sineminyaka engaphezu kwe-15 yamava ekwenziweni nasekuthumeleni kumazwe angaphandle uluhlu olubanzi oluphezulu lwamayeza aphakathi okanye amachiza alungileyo.
Iimarike eziphambili?Thengisa kwimarike yasekhaya, eMntla Melika, eYurophu, eIndiya, eKorea, eJapan, eOstreliya, njl.
Iingenelo?Umgangatho ophezulu, ixabiso elifikelelekayo, iinkonzo zengcali kunye nenkxaso yobugcisa, ukuhanjiswa ngokukhawuleza.
UmgangathoIsiqinisekiso?Inkqubo yokulawula umgangatho ongqongqo.Izixhobo zobuchwephesha zokuhlalutya ziquka i-NMR, LC-MS, GC, HPLC, ICP-MS, UV, IR, OR, KF, ROI, LOD, MP, Clarity, Solubility, Microbial limit test, njl.
Iisampulu?Uninzi lweemveliso zibonelela ngeesampulu zasimahla zokuvavanya umgangatho, iindleko zokuthumela kufuneka zihlawulwe ngabathengi.
Factory Audit?Uphicotho-zincwadi lwasefektri wamkelekile.Nceda wenze idinga kwangaphambili.
MOQ?Akukho MOQ.Umyalelo omncinci wamkelekile.
Ixesha lokuzisa? Ukuba ngaphakathi kwesitokhwe, ukuhanjiswa kweentsuku ezintathu kuqinisekisiwe.
Ezothutho?Nge-Express (FedEx, DHL), ngoMoya, ngoLwandle.
Amaxwebhu?Emva kwenkonzo yokuthengisa: I-COA, i-MOA, i-ROS, i-MSDS, njl.
Udibaniso lweSiko?Inokubonelela ngeenkonzo zesiko lokudibanisa ukuze zilungele iimfuno zakho zophando.
Immimiselo yokuhlawula?I-invoyisi yeProforma iya kuthunyelwa kuqala emva kokuqinisekiswa kwe-odolo, efakwe kwiinkcukacha zethu zebhanki.Intlawulo nge-T / T (i-Telex Transfer), i-PayPal, i-Western Union, njl.
Iimpawu zeHazard Xn - Ziyingozi
Iikhowudi zoMngcipheko R37/38 - Ukucaphukisa kwinkqubo yokuphefumla kunye nolusu.
R41 - Umngcipheko womonakalo omkhulu emehlweni
I-R42/43 - Inokubangela uvakalelo ngokuphefumla kunye nokudibana nolusu.
I-R62 - Umngcipheko onokubakho wokuphazamiseka kokuchuma
R68 - Umngcipheko onokubakho weziphumo ezingajikiyo
R40 - Ubungqina obuncinci besiphumo somhlaza
I-R48 - Ingozi yomonakalo omkhulu kwimpilo ngokuba sesichengeni ixesha elide
I-R20/21/22 - Iyingozi ngokuphefumla, xa udibana nolusu naxa uginyiwe.
R68/20/21/22 -
Inkcazelo yoKhuseleko S22 - Musa ukuphefumla uthuli.
S26 - Xa udibana namehlo, hlambulula ngokukhawuleza ngamanzi amaninzi kwaye ufune iingcebiso zonyango.
S36/37/39 - Nxiba iimpahla ezifanelekileyo zokukhusela, iiglavu kunye nokukhusela amehlo / ubuso.
S45 - Kwimeko yengozi okanye ukuba uziva ungaphilanga, funa ingcebiso kagqirha ngokukhawuleza (bonisa ileyibhile nanini na kunokwenzeka.)
Ii-ID ze-UN 1544
WGK eJamani 3
RTECS DA8340700
FLUKA BRAND F IIKHOWUDI 10-21
Ikhowudi yeHS 2932999021
Udidi lweeNgozi 6.1(b)
Ukupakisha Iqela III
Ubuthi LD50 intraperitoneal kwi mouse: 128mg/kg
I-Paclitaxel (i-Taxol) (i-CAS: i-33069-62-4), imveliso yendalo eyodwa kwi-bark ye-Pacific yew, iyasebenza ekuphatheni i-refractory metastatic ovarian cancer.Ngokungafaniyo nayiphi na enye i-antineoplastic agents, i-paclitaxel ibonakala ineendlela ezininzi ezinokuthi zenziwe, kubandakanywa isenzo se-antimicrotubule ngokukhuthazwa kwe-polymerization ye-tubulin kunye nokuqiniswa kwe-microtubules, ngaloo ndlela, ukumisa i-mitosis kunye nokukhuthaza ukufa kweeseli.Unikezelo lwe-paclitaxel luthintelwe bubuninzi bayo bendalo obuphantsi kwaye ngoku iveliswa ngendlela elungelelanisiweyo ukusuka kwi-deacetylbaccatin Ⅲ ebekwe yodwa kwiinaliti zomthi we-yew.Ukugqitywa kutsha nje kweendlela ezimbini ezidityanisiweyo zetaxol zoyisile ukuntsonkotha kwesakhiwo sekhompawundi yesihloko kwaye kunokuba luncedo ekufumaneni ii-analog ezithile ezisondeleleneyo ezisondeleleneyo, ezifunyaniswe zinento yokwenza ne-antitumor.I-Paclitaxel inokusetyenziswa kunyango lomhlaza webele we-metastatic, umhlaza wemiphunga, umhlaza wentloko kunye nentamo, kunye ne-melanoma eyingozi.
Izithako eziyityhefu kumasebe kunye namagqabi e-Taxus chinensis zohlulwa ngo-1856 zaze zabizwa ngokuba yi-“taxine,” eyachongwa njengodidi lwecandelo le-alkaloid emhlophe.Okwangoku, phakathi kwawo onke amachiza e-antitumor, ukuthengiswa kwe-paclitaxel kuba yeyokuqala kwihlabathi njengeyeza elaziwayo le-anticancer elinomsebenzi onamandla obanzi.Ngo-Okthobha we-1995, i-China yaba lilizwe lesibini kunye nemveliso esemthethweni ye-paclitaxel kunye nenaliti yayo emhlabeni.Impumelelo yafunyanwa phantsi kwemizamo engagungqiyo yabaphandi kwiZiko leMateria Medica, iChinese Academy yeSayensi yezoNyango.
I-Paclitaxel (i-CAS: i-33069-62-4) i-antineoplastic esetyenziselwa ukunyanga izigulane ezinemiphunga, i-ovarian, umhlaza webele, intloko kunye nomhlaza wentamo, kunye neendlela eziphambili ze-Kaposi's sarcoma.I-Paclitaxel yi-mitotic inhibitor esetyenziswa kwi-chemotherapy yomhlaza.Ikwasetyenziswa kwisifundo sesakhiwo kunye nomsebenzi we-microtubles kwi-tubulin.
I-Paclitaxel inefuthe elihle kumhlaza we-ovarian we-refractory kunye nomhlaza webele kunye nokuxhatshazwa kweziyobisi ezifana nomhlaza we-ovarian kunye neplatinam, kunye nethemba elihle lokunyanga umhlaza we-prostate, umhlaza wentloko kunye nentamo, umhlaza we-esophageal, i-germ cell tumor, umhlaza we-endometrial, i-lymphoma, umhlaza wesinyi, umhlaza womgudu wokwetyisa ongentla, iseli encinci kunye nomhlaza wemiphunga weseli ongeyonxalenye encinci.
I-Paclitaxel (i-Taxol) (i-CAS: i-33069-62-4) iyinkimbinkimbi kakhulu, i-organic compound eyodwa kwi-bark ye-Pacific yew tree.Ibophelela kwi-tubulin dimers kunye ne-microtubulin filaments, ukukhuthaza ukuhlanganiswa kwee-filaments kunye nokuthintela ukuchithwa kwazo.Oku kunyuka kokuzinza kwe-microfilaments kubangela ukuphazamiseka kwe-mitosis kunye ne-cytotoxicity kwaye kuphazamise ezinye izinto eziqhelekileyo ze-microtubular, ezifana nokuthuthwa kwe-axonal kwi-nerve fibers.Eyona ndlela iphambili yokuxhathisa echongiwe i-paclitaxel kukuhanjiswa ngaphandle kweeseli zethumba, nto leyo ekhokelela ekwehleni kokuqokelelwa kweziyobisi kwi-intracellular.Olu hlobo lokuchasana luxutywe ngumthuthi we-multidrug transporter P-glycoprotein.
Isenokuba nobuntununtunu kutyhileko olude lokufuma.
