Crenolanib

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

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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

分子量

443.54

储存条件

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

体外

Ethanol

7mg/mL(15.78mM)

DMSO

88mg/ml(198.4 mM)

Water

<1mg/ml

体内

30% PEG400+0.5% Tween80+5% propylene glycol

30 mg/mL

* <1 mg/ml refers to the product slightly soluble or insoluble

浓度溶解体积质量

1mg

5mg

10mg

1mM