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DCC-2036 (rebastinib) is an Abl inhibitor that exhibits anticancer activity. In cellular models of chronic myelogenous leukemia (CML), rebastinib induces apoptosis and inhibits cell proliferation. Rebastinib binds the switch control pocket of Abl that is involved in conformational regulation of the kinase domain.
| Cas No. | 1020172-07-9 |
|---|---|
| Purity | ≥98% |
| Formula | C30H28FN7O3 |
| Formula Wt. | 553.59 |
| IUPAC Name | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide |
| Synonym | DCC2036, Rebastinib |
| Solubility | DMSO 111 mg/mL (200.5 mM) Ethanol 16 mg/mL (28.9 mM) Water Insoluble |
| Appearance | White to off white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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| Info Sheet |
Shen Y, Shi X, Pan J. The conformational control inhibitor of tyrosine kinases DCC-2036 is effective for imatinib-resistant cells expressing T674I FIP1L1-PDGFRα. PLoS One. 2013 Aug 29;8(8):e73059. PMID: 24009732.
Eide CA, Adrian LT, Tyner JW, et al. The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile. Cancer Res. 2011 May 1;71(9):3189-95. PMID: 21505103.