生物活性
Product Description
Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src.
Target
PDGFRβ
PDGFRα
View more
IC50 Value
3.2nM(Kd)
2.1nM(Kd)
Diseases and Conditions
Cancer
体外
Crenolanib是一种口服具有生物活性的,高度有效的,选择性PDGFR TKI。Crenolanib是苯并咪唑化合物,对PDGFRA和PDGFRB的IC50s分别为0.9 nM和1.8 nM。Crenolanib明显比伊马替尼有效,能够抑制对伊马替尼耐药的PDGFRα激酶(D842I,D842V,D842Y,D1842-843IM,和缺失I843)活性。Crenolanib作用于同基因模型系统中D842V,比伊马替尼有效135倍,IC50大约为10 nM。Crenolanib抑制EOL-1细胞中融合致癌基因的激酶活性,其衍生自慢性噬酸细胞白血病患者,且表达持续活化的FIP1L1- PDGFRα融合激酶,IC50 = 21 nM。Crenolanib也会抑制EOL-1细胞的增殖,IC50 = 0.2 pM。Crenolanib抑制在BaF3细胞中表达的V561D或D842V突变激酶的活化,IC50分别为85 nM或272 nM。Crenolanib抑制H1703非小细胞肺癌细胞系中PDGFRα活化,其能够使包含PDGFRα基因座的4q12区域扩增24倍,IC50为26 nM。
体内
Chemical information:
分子量
443.54
储存条件
3 years -20 ℃ powder
2 years -80 ℃ In solvent
分子式
C26H29N5O2
CAS:
670220-88-9
备注
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
溶解度
Ethanol
7mg/mL(15.78mM)
DMSO
88mg/ml(198.4 mM)
Water
<1mg/ml
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL
* <1 mg/ml refers to the product slightly soluble or insoluble
制备储备液
浓度溶解体积质量
1mg
5mg
10mg
1mM
TargetMol中国(陶术生物)
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