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Product Details

Crenolanib | PDGFR and FLT3 inhibitor

Crenolanib (670220-88-9) is a potent inhibitor of PDGFR (Kd for α = 2.1 nM; β = 3.2 nM) and FLT3 (Kd = 0.74 nM).1 Crenolanib is a type I inhibitor binding only to the active kinase conformation. It showed potent activity against imatinib-resistant PDGFRα mutations D842I, D842V, D842Y, DI842-843M, and deletion I8432 as well as FLT3/ITD and FLT3/D835 mutants3. Crenolanib acted synergistically with FLT3-CAR T-cells in a FLT3-ITD+ AML murine xenograft model.4

References/Citations
1) Lewis et al. (2009) Phase I study of the safety, tolerability, and pharmacokinetics of oral CP-868,596, a highly specific platelet-derived growth factor receptor tyrosine kinase inhibitor in patients with advanced cancers; J. Clin. Oncol. 27 5262
2) Smith et al. (2014) Crenolanib is a selective type I pan-FLT3 inhibitor; Proc. Natl. Acad. Sci. USA 111 5319
3) Heinrich et al. (2012) Crenolanib Inhibits Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors; Clin. Cancer Res. 18 4375
4) Jetani et al. (2018) CAR T-cells targeting FLT3 have potent activity against FLT-ITD+ AML and act synergistically with the FLT3-inhibitor crenolanib; Leukemia 32 1168

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Catalog#  10-4782-0005

$60.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
670220-88-9
Catalog Number:
10-4782
Activity:
PDGFR and FLT3 inhibitor
Chemical Name:
1-[2-[5-[(3-Methyloxetan-3-yl)methoxy]benzimidazole-1-yl]quinoline-8-yl]piperidin-4-amine
Alternate Name:
CP-868,596
Molecular Weight:
443.55
Molecular Formula:
C26H29N5O2
Solubility:
Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 10 mg/ml).
Physical Properties:
White solid
Purity:
97% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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