Suninib (CAS# 557795-19-4) Featured Image

Suntinib (CAS# 557795-19-4)

Chemical Property:

Molecular Formula	C22H27FN4O2
Molar Misa	398.47
Density	1.2
Melting Point	189-191°C
Boling Point	572.1±50.0 °C(Zvakafanotaurwa)
Flash Point	299.8℃
Solubility	25°C: DMSO
Vapor Presure	3.13E-23mmHg pa25°C
Chitarisiko	Crystalline upfu
Color	Yero kusvika kuRima Orange
pKa	8.5(pa25℃)
Storage Condition	2-8°C
MDL	MFCD08273555
In vitro kudzidza	Sunitinib inoshanda mukudzivisa Kit uye FLT-3. Sunitinib inoshanda ATP inokwikwidza inhibitor yeVEGFR2 (Flk1) uye PDGFRβ, KI iri 9 nM uye 8 nM zvakateerana, kuita paVEGFR2 uye PDGFR inoshanda kupfuura FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, uye src kusarudzwa kwaive kwakapfuura 10 nguva dzakakwirira. Mune serum-nzara NIH-3T3 masero anoratidza VEGFR2 kana PDGFRβ, Sunitinib inhibited VEGF-inotenderera VEGFR2 phosphorylation uye PDGF-inotenderera PDGFRβ phosphorylation ine IC50 ye10 nM uye 10 nM, maererano. Kune NIH-3T3 masero akawandisa PDGFRβ kana PDGFRα, Sunitinib yakadzivisa kupararira kunokonzerwa neVEGF neIC50 ye39 nM uye 69 nM, maererano. Sunitinib inhibited wild-type FLT3,FLT3-ITD, uye FLT3-Asp835 phosphorylation ine IC50 ye250 nM,50 nM, uye 30 nM, zvichiteerana. Sunitinib yakadzivisa kuwanda kweMV4; 11 uye OC1-AML5 masero ane IC50 ye8 nM uye 14 nM, zvichiteerana, uye yakakonzera apoptosis nenzira inoenderana nedosi.
In vivo kudzidza	Zvinoenderana neyakakura, yakasarudzika inhibition yephosphorylation uye kusaina kweVEGFR2 kana PDGFR muvivo, Sunitinib (20-80 mg/kg/zuva) yakaratidzwa kuve inokonzera akasiyana siyana tumor xenograft modhi, kusanganisira HT-29, A431, Colo205, h. -460, SF763T,C6,A375, kana MDA-MB-435 yakaratidza zvakanyanya simba-inotsamira antitumor chiitiko. Suninib pachiyero che 80 mg / kg / zuva kwemazuva 21 yakaguma nekuzara kwebundu regression mu6 ye8 mice, uye pakupera kwekurapa, zvipembenene hazvina kudzoka zvakare munguva yekucherechedza kwemazuva e110. Rwendo rwechipiri rwekurapa neSunitinib rwakanga ruchiri kushanda pakurwisa mamota, asi harina kupora kubva pachikamu chekutanga chekurapa. Kurapa kweSunitinib kwakaguma nekuderera kukuru kwebundu MVD, iyo yakaderedzwa ne ~ 40% muSF763T gliomas. Kurapa kweSU11248 kwakaguma nekuvharwa kwakazara kwekuwedzera bundu kukura kweluciferase-inoratidza PC-3M xenografts, kunyangwe pakanga pasina kuderedzwa kwekukura kwebundu. Mune FLT3-ITD bone marrow transplantation model, Sunitinib kurapwa (20 mg / kg / zuva) yakadzivisa zvakanyanya kukura kwe subcutaneous MV4; 11 (FLT3-ITD) xenografts uye kurarama kwenguva refu.