Crenolanib (CP-868596) | PDGFR/FLT-3 inhibitor

Chemical Structure : Crenolanib

CAS No.: 670220-88-9

Crenolanib (CP-868596, CP868596)

Catalog No.: 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.

Packing	Price	Stock
5 mg	$78	In stock
10 mg	$118	In stock
25 mg	$218	In stock
50 mg	$358	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	443.5408
Formula	C26H29N5O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-Piperidinamine, 1-[2-[5-[(3-methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]-

References

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.

Crenolanib (CP-868596, CP868596)

Biological Activity

Physicochemical Properties

References

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