Product Description
CP868596 (Crenolanib) is an orally-available, benzimidazole-based inhibitor of PDGFRa and PDGFRb with IC50 values of 0.9 and 1.8 nM, respectively. Furthermore, CP868596 is active against the D842V mutant of PDGFRa, inhibiting phosphorylation at an IC50 range of 10-30 nM (wild-type PDGFRa IC50 = 10 nM). [1] Whereas imatinib, sunitinib, sorafenib, and nilotinib have little to no activity vs. this D842V mutant, CP868596 offers a novel therapy to GIST patients with this resistance.CP868596 also shows potency (IC50 = 80 nM) against the highly sensitive H1703 cell line, suggesting single-agent therapy potential for PDGFR-driven NSCLC tumors. [2]
Technical information:
| Chemical Formula: | C26H29N5O2 | |
| CAS #: | 670220-88-9 | |
| Molecular Weight: | 443.54 | |
| Purity: | >98% | |
| Appearance: | White | |
| Chemical Name: | 1-(2-(5-((3-methyloxetan-3-yl)methoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | CP-868569, CP 868596, CP868569, Crenolanib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature. Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | \"Crenolanib (CP-868,596), a Highly Potent PDGFR Inhibitor, Inhibits Phosphorylation of the Imatinib-Resistant PDGFR? (D842V) Activating Mutation Associated with Advanced GIST\" AROG Pharmaceuticals and Oregon Health & Science University, AACR poster, 2011, Abstract 3586. |
| 2. | \"Crenolanib (CP-868,596), a highly potent and selective PDGFR TKI inhibits growth of PDGFR?-driven lung cancer cells\" AROG Pharmaceuticals and Southwestern Medical Center, AACR poster, 2011, Abstract 3601. |
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