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Sunitinib（CAS# 557795-19-4) Ki‘i Hō‘ike‘ike
  • Sunitinib（CAS# 557795-19-4) 1

Sunitinib（CAS# 557795-19-4)

Waiwai Kemika:

ʻĀpana Molekala C22H27FN4O2
Molar Mass 398.47
ʻO ka mānoanoa 1.2
Lae hehee 189-191°C
Lae Boling 572.1±50.0 °C(Wanamua)
Lae Flash 299.8 ℃
Ka hoʻoheheʻe 25°C: DMSO
Puʻupuʻu mahu 3.13E-23mmHg ma 25°C
Ka nana aku Ka pauda kristal
kala kala Melemele a ʻAlani ʻeleʻele
pKa 8.5 (ma 25 ℃)
Kūlana Waihona 2-8°C
MDL MFCD08273555
Haʻawina in vitro He mea maikaʻi ʻo Sunitinib i ka pale ʻana i ka Kit a me FLT-3. ʻO Sunitinib kahi mea hoʻokūkū hoʻokūkū ATP maikaʻi o VEGFR2 (Flk1) a me PDGFRβ, ʻo KI ka 9 nM a me 8 nM pākahi, e hana ana ma VEGFR2 a ʻoi aku ka maikaʻi o ka PDGFR ma mua o FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, a ʻOi aku ka nui o nā koho src ma mua o 10 mau manawa kiʻekiʻe. I loko o nā pūnaewele NIH-3T3 pōloli serum e hōʻike ana i ka VEGFR2 a i ʻole PDGFRβ, ua kāohi ʻo Sunitinib i ka VEGF-dependent VEGFR2 phosphorylation a me ka PDGF-dependent PDGFRβ phosphorylation me kahi IC50 o 10 nM a me 10 nM. No nā pūnaewele NIH-3T3 e hōʻike nui ana i ka PDGFRβ a i ʻole PDGFRα, ua kāohi ʻo Sunitinib i ka hoʻonui ʻia e VEGF me kahi IC50 o 39 nM a me 69 nM. Ua kāohi ʻo Sunitinib i ka FLT3, FLT3-ITD, a me FLT3-Asp835 phosphorylation me IC50 o 250 nM, 50 nM, a me 30 nM. Ua kāohi ʻo Sunitinib i ka hoʻonui ʻana o nā pūnaewele MV4; 11 a me OC1-AML5 me IC50 o 8 nM a me 14 nM, i kēlā me kēia, a hoʻokomo i ka apoptosis ma ke ʻano pili.
In vivo haʻawina Kūlike me ka nui, koho koho o ka phosphorylation a me ka hōʻailona o VEGFR2 a i ʻole PDGFR i vivo, ua hōʻike ʻia ʻo Sunitinib (20-80 mg / kg / lā) i ke kuleana no nā ʻano like ʻole xenograft tumor, me HT-29, A431, Colo205, h -460, SF763T, C6, A375, a i ʻole MDA-MB-435 i hōʻike ʻia ka nui o ka hana antitumor pili i ka dosis. ʻO Sunitinib ma kahi maʻi o 80 mg / kg / lā no nā lā 21 i hopena i ka regression tumo piha i ka 6 o 8 mauʻiole, a ma ka hopena o ka mālamaʻana,ʻaʻole i hoʻoulu hou nā maʻi koko i ka manawa o ka nānāʻana i nā lā 110. ʻO ka lua o ka lāʻau lapaʻau me Sunitinib ua maikaʻi nō ia e kūʻē i nā maʻi maʻi, akā ʻaʻole i ola maikaʻi mai ka pōʻai mua o ka mālama ʻana. ʻO ka mālama ʻana iā Sunitinib ka hopena i ka emi nui o ka MVD tumo, i hoʻemi ʻia e ~ 40% ma SF763T gliomas. ʻO ka mālama ʻana ʻo SU11248 ka hopena i ka pale piha ʻana i ka ulu ʻana o ka tumo hou o nā xenografts PC-3M e hōʻike ana i ka luciferase, ʻoiai ʻaʻole i hōʻemi ʻia ka nui o ka tumora. I loko o ka FLT3-ITD hoʻololi ʻana i ka iwi iwi iwi, ʻo ka mālama ʻana iā Sunitinib (20 mg/kg/lā) i kāohi nui i ka ulu ʻana o nā xenografts subcutaneous MV4; 11 (FLT3-ITD) a me ke ola lōʻihi.

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Ka wehewehe palekana 24/25 - E pale i ka pili ʻana me ka ʻili a me nā maka.
HS Code 29337900

 

Hoʻolauna

ʻO Sunitinib kahi mea hoʻopiʻi RTK multi-target e kuhikuhi ana iā VEGFR2 (Flk-1) a me PDGFRβ me IC50 o 80 nM a me 2 nM, a ke kāohi pū nei hoʻi i ka c-Kit.

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