Crenolanib
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Crenolanib
CAS No. : 670220-88-9
MCE 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 Kd 分别为 0.74 nM,2.1 nM,3.2 nM。
研究领域:Protein Tyrosine Kinase/RTK | 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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Reprogramming Compound Library | Anti-COVID-19 Compound Library | Anti-Lung Cancer Compound Library | Anti-Blood Cancer Compound Library | Sunitinib | Imatinib | SU 5402 | Cediranib | AT9283 | Gandotinib | KW-2449 | Lestaurtinib | CG-806 | AST 487 | Ki20227 | SU14813 | PP121 | Sennoside B | PP58 | AG 1295 | JNJ-47117096 hydrochloride | Methylnissolin | BPR1J-097 Hydrochloride | Crotonoside | SU16f | Trapidil | Tyrosine kinase-IN-1 | SKLB4771 | Tyrphostin AG1296 | Tyrphostin AG1433 | NVP-ACC789 | PD-161570
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