N-Desethyl Sunitinib 是 Sunitinib 的代谢物。其中Sunitinib是有效的以及ATP 竞争的VEGFR、PDGFRβ和KIT抑制剂,能够抑制 VEGFR -1 (Ki:2 nM) 、VEGFR-2 (Ki:9 nM) 、VEGFR-3 (Ki:17 nM) 、PDGFRβ (Ki:8 nM) 、KIT (Ki:4 nM) 的活性。
产品描述
N-Desethyl Sunitinib is a sunitinib metabolite.
体外活性
Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner[1].Sunitinib also potently inhibits Kit and FLT-3[3].
体内活性
Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model[1].
Cas No.
356068-97-8
分子式
C20H23FN4O2
分子量
370.42
别名
N-去乙基-舒尼替尼;SU-11662
储存和溶解度
DMSO:50 mg/mL (134.98 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years