Crenolanib
Cat. No.:YN440254
产品名称: | Crenolanib |
CAS No.: | 670220-88-9 |
Chemical Name: | 1-[2-[5-[(3-methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]-4-piperidinamine |
Synonyms: | CP-868596 |
分子量: | 443.54 |
分子式: | C₂₆H₂₉N₅O₂ |
SMILES: | NC1CCN(C2=CC=CC3=C2N=C(N4C5=CC=C(C=C5N=C4)OCC6(COC6)C)C=C3)CC1 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | 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。 |
IC50和靶点: | [{name:"PDGFRα:2.1 nM (Kd)"},{name: "PDGFRβ:3.2 nM (Kd)"},{name: "FLT3:0.74 nM (Kd)"}] |
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Heinrich, M.C., Griffith, D., McKinley, A., et al.Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumorsClin. Cancer Res.18(16),4375-4385(2012)
Smith, C.C., Lasater, E.A., Lin, K.C., et al.Crenolanib is a selective type I pan-FLT3 inhibitorProc. Natl. Acad. Sci. USA111(14),5319-5324(2014)
Dai, J., Kong, Y., Si, L., et al.Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanibClin. Cancer Res.19(24),6935-6942(2013)
Galanis, A., Ma, H., Rajkhowa, T., et al.Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutantsBlood123(1),94-100(2014)