Sunitinib (CAS# 557795-19-4)

Abubuwan Sinadarai:

Tsarin kwayoyin halitta	Saukewa: C22H27FN4O2
Molar Mass	398.47
Yawan yawa	1.2
Matsayin narkewa	189-191 ° C
Matsayin Boling	572.1 ± 50.0 °C (An annabta)
Wurin Flash	299.8 ℃
Solubility	25°C: DMSO
Tashin Turi	3.13E-23mmHg a 25°C
Bayyanar	Crystalline foda
Launi	Yellow zuwa Orange Dark
pKa	8.5 (a 25 ℃)
Yanayin Ajiya	2-8 ° C
MDL	Saukewa: MFCD0827355
Nazarin in vitro	Sunitinib yana da tasiri wajen hana Kit da FLT-3. Sunitinib shine ingantacciyar mai hanawa ATP gasa na VEGFR2 (Flk1) da PDGFRβ, KI shine 9 nM da 8 nM bi da bi, yin aiki akan VEGFR2 kuma PDGFR yafi inganci fiye da FGFR-1,EGFR, Cdk2, Met, IGFR-1, Abl, da Zaɓuɓɓukan src sun kasance sama da sau 10 mafi girma. A cikin ƙwayoyin NIH-3T3 masu fama da yunwa da ke bayyana VEGFR2 ko PDGFRβ, Sunitinib ya hana VEGF-dogara VEGFR2 phosphorylation da PDGF-dogara PDGFRβ phosphorylation tare da IC50 na 10 nM da 10 nM, bi da bi. Don ƙwayoyin NIH-3T3 da ke wuce gona da iri PDGFRβ ko PDGFRa, Sunitinib ya hana haɓakar da VEGF ta haifar tare da IC50 na 39 nM da 69 nM, bi da bi. Sunitinib ya hana nau'in daji FLT3,FLT3-ITD, da FLT3-Asp835 phosphorylation tare da IC50 na 250 nM,50 nM, da 30 nM, bi da bi. Sunitinib ya hana yaduwar ƙwayoyin MV4;11 da OC1-AML5 tare da IC50 na 8 nM da 14 nM, bi da bi, kuma ya haifar da apoptosis a cikin hanyar dogara da kashi.
A cikin nazarin vivo	Daidai da mahimmanci, zaɓin hanawa na phosphorylation da siginar VEGFR2 ko PDGFR a cikin vivo, Sunitinib (20-80 mg / kg / day) an nuna yana da alhakin nau'ikan xenograft iri-iri, gami da HT-29, A431, Colo205, h -460, SF763T, C6, A375, ko MDA-MB-435 ya baje kolin ayyukan antitumor masu dogaro da yawa. Sunitinib a kashi na 80 mg / kg / rana na kwanaki 21 ya haifar da cikakkiyar farfadowa a cikin 6 na 8 mice, kuma a ƙarshen jiyya, ciwace-ciwacen daji ba su sake farfadowa ba a lokacin lura na kwanaki 110. A zagaye na biyu na jiyya tare da Sunitinib har yanzu yana da tasiri a kan ciwace-ciwacen daji, amma bai warke sosai daga zagaye na farko na jiyya ba. Maganin Sunitinib ya haifar da raguwa mai yawa a cikin ƙwayar ƙwayar cuta MVD, wanda aka rage ta ~ 40% a cikin SF763T gliomas. SU11248 jiyya ya haifar da cikakken hana ƙarin haɓakar ƙwayar ƙwayar cuta na luciferase-bayyana PC-3M xenografts, kodayake babu raguwa a girman ƙwayar cuta. A cikin FLT3-ITD kasusuwan kasusuwa na kasusuwa, magani na Sunitinib (20 mg / kg / day) ya hana ci gaban MV4 na subcutaneous; 11 (FLT3-ITD) xenografts da kuma tsawon rayuwa.