I-Sunitinib (CAS# 557795-19-4)

Isakhiwo Samakhemikhali:

I-Molecular Formula	I-C22H27FN4O2
I-Molar Mass	398.47
Ukuminyana	1.2
I-Melting Point	189-191°C
I-Boling Point	572.1±50.0 °C(Kubikezelwe)
I-Flash Point	299.8℃
Ukuncibilika	25°C: DMSO
I-Vapor Presure	3.13E-23mmHg ku-25°C
Ukubukeka	I-Crystalline powder
Umbala	Okuphuzi ukuya kokuwolintshi Okumnyama
pKa	8.5(ku-25℃)
Isimo Sesitoreji	2-8°C
I-MDL	MFCD08273555
Isifundo se-in vitro	I-Sunitinib iyasebenza ekuvimbeleni i-Kit ne-FLT-3. I-Sunitinib iyi-ATP ephumelelayo yokuncintisana inhibitor ye-VEGFR2 (Flk1) ne-PDGFRβ, i-KI ingu-9 nM no-8 nM ngokulandelanayo, isebenza ku-VEGFR2 kanye ne-PDGFR iphumelela kakhulu kune-FGFR-1, EGFR, Cdk2, Met,IGFR-1, Abl, kanye Ukukhetha kwe-src bekungaphezulu kwezikhathi eziyi-10 ngaphezulu. Kumaseli e-NIH-3T3 abulawa yi-serum aveza i-VEGFR2 noma i-PDGFRβ, i-Sunitinib ivimbele i-VEGF-dependent VEGFR2 phosphorylation kanye ne-PDGF-phosphorylation ye-PDGFRβ ene-IC50 ye-10 nM kanye ne-10 nM, ngokulandelanayo. Kumaseli e-NIH-3T3 aveza ngokweqile i-PDGFRβ noma i-PDGFRα, i-Sunitinib ivimbele ukwanda okubangelwa i-VEGF nge-IC50 ye-39 nM kanye ne-69 nM, ngokulandelanayo. I-Sunitinib inhibited wild-type FLT3,FLT3-ITD, kanye ne-FLT3-Asp835 phosphorylation ne-IC50 ye-250 nM,50 nM, kanye ne-30 nM, ngokulandelanayo. I-Sunitinib ivimbele ukwanda kwamaseli e-MV4;11 kanye ne-OC1-AML5 ane-IC50 ye-8 nM kanye ne-14 nM, ngokulandelana, futhi yenze i-apoptosis ngendlela encike kumthamo.
Isifundo se-vivo	Ngokuhambisana nokuvinjwa okukhulu, okukhethiwe kwe-phosphorylation kanye nokusayina kwe-VEGFR2 noma i-PDGFR ku-vivo, i-Sunitinib (20-80 mg/kg/ngosuku) ikhonjiswe ukuthi inesibopho samamodeli ahlukahlukene we-tumor xenograft, okuhlanganisa i-HT-29, A431, Colo205, h. -460, SF763T,C6,A375, noma I-MDA-MB-435 ibonise umsebenzi we-antitumor oncike kumthamo onamandla kakhulu. I-Sunitinib kumthamo we-80 mg / kg / ngosuku ngezinsuku ze-21 ibangele ukuhlehliswa okuphelele kwe-tumor ku-6 yamagundane we-8, futhi ekupheleni kokwelashwa, izimila azizange zivuseleleke phakathi nesikhathi sokubuka kwezinsuku ze-110. Umzuliswano wesibili wokwelashwa nge-Sunitinib wawusasebenza ngokumelene nezimila, kodwa awuzange ululame ngokugcwele emzuliswaneni wokuqala wokwelashwa. Ukwelashwa kwe-Sunitinib kubangele ukwehla okuphawulekayo kwe-tumor MVD, eyehliswa ngo-~ 40% kuma-gliomas e-SF763T. Ukwelashwa kwe-SU11248 kubangele ukuvinjelwa okuphelele kokukhula kwe-tumor eyengeziwe ye-luciferase-eveza i-PC-3M xenografts, nakuba kungekho kuncipha kosayizi wesimila. Kumodeli yokufakelwa kwamathambo e-FLT3-ITD, ukwelashwa kwe-Sunitinib (20 mg/kg/ngosuku) kuvimbe kakhulu ukukhula kwe-subcutaneous MV4;11 (FLT3-ITD) xenografts kanye nokuphila isikhathi eside.