Chemical Structure : Crenolanib
CAS No.: 670220-88-9
货号: PC-43403Not For Human Use, Lab Use Only.
Crenolanib (CP-868596) is a potent, selective PDGFR/Flt-3 inhibitor with Ki of 3.2, 2.1 and 0.74 nM for wild-type PDGFRα, PDGFRβ and FLT3, respectively.
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---|---|---|---|
5 mg | ¥780 | In stock | |
10 mg | ¥1180 | In stock | |
25 mg | ¥2180 | In stock | |
50 mg | ¥3580 | In stock | |
100 mg | Get quote |
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Crenolanib (CP-868596) is a potent, selective PDGFR/Flt-3 inhibitor with Ki of 3.2, 2.1 and 0.74 nM for wild-type PDGFRα, PDGFRβ and FLT3, respectively.
Crenolanib (CP-868596) displays >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src.
Crenolanib (CP-868596) also is a potent inhibitor of PDGFRα D842V-mutant kinase with IC50 of 10 nM, significantly more potent than imatinib in inhibiting the kinase activity of imatinib-resistant PDGFRA kinases (D842I, D842V, D842Y, DI842-843IM, and deletion I843).
Crenolanib is active against models of drug-resistant FLT3-ITD-positive AML.
分子量 | 443.5408 | |
分子式 | C26H29N5O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
4-Piperidinamine, 1-[2-[5-[(3-methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]- |
1. Heinrich MC, et al. Clin Cancer Res. 2012 Aug 15;18(16):4375-84.
2. Zimmerman EI, et al. Blood. 2013 Nov 21;122(22):3607-15.
3. Galanis A, et al. Blood. 2014 Jan 2;123(1):94-100.
4. Smith CC, et al. Proc Natl Acad Sci U S A. 2014 Apr 8;111(14):5319-24.
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