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Crenolanib

CAS No. : 670220-88-9

MCE 国际站：Crenolanib

产品活性：Crenolanib 是有效和选择性的野生型和突变型 III 类受体酪氨酸激酶抑制剂，抑制 FLT3 和 PDGFRα/β 的 K_d 分别为 0.74 nM，2.1 nM，3.2 nM。

研究领域：Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶点：FLT3  |  PDGFR  |  Autophagy

In Vitro: Crenolanib has 25-fold more affinity for PDGFRA/B compared with KIT, and is approximately 135-fold more potent than STI571 for inhibiting the PDGFRA D842V mutation. The IC₅₀ for crenolanib for a KIT exon 11 deletion mutant kinase is greater than 1,000 versus 8 nM for STI571. Crenolanib has low nanomolar potency against the V561D + D842V-mutant kinase that is similar to its potency against the isolated D842V mutation. Both STI571 and crenolanib potently inhibit the kinase activity of the fusion oncogene with IC₅₀ values of 1 and 21 nM, respectively, and inhibits PDGFRA activation in this cell line with IC₅₀ values of 93 and 26 nM, respectively. HL60/VCR and K562/ABCB1 cells, overexpressing ABCB1, are 6.9- and 3.6-fold resistant to crenolanib, respectively, in relation to parental HL60 and K562 cells. PSC-833 fully reverses resistance to crenolanib in both HL60/VCR and K562/ABCB1 cells. Crenolanib (1 nM-10 μM) stimulates ABCB1 ATPase activity in a concentration-dependent manner. Crenolanib treatment does not increase the cell surface expression of ABCB₁. Crenolanib inhibits [¹²⁵I]-IAAP photocrosslinking of ABCB1 at high concentrations, with 50 % inhibition at 10 μM, but has little effect at lower concentrations, below 1 μM. Crenolanib decreases NSCLC cell viability, induces apoptosis in NSCLC cells, and inhibits cell migration in NSCLC cells.

In Vivo: Crenolanib (10 mg/kg and 20 mg/kg) suppresses non-small-cell lung cancer tumor growth in vivo and induces tumor cell apoptosis, and the dosage of crenolanib applied is well tolerated by recipient mice.

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