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Chemical Structure : DCC-2036
CAS No.: 1020172-07-9
Catalog No.: PC-43334Not For Human Use, Lab Use Only.
DCC-2036 (Rebastinib) is a highly potent, non-ATP-competitive BCR-ABL1 inhibitor with IC50 of 0.8 and 4 nM for native ABL1 and gatekeeper mutant ABL1 T315I, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg (Free Sample) | $28 | In stock | |
| 10 mg | $118 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $328 | In stock | |
| 100 mg | Get quote |
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DCC-2036 (Rebastinib) is a highly potent, non-ATP-competitive BCR-ABL1 inhibitor with IC50 of 0.8 and 4 nM for native ABL1 and gatekeeper mutant ABL1 T315I, respectively.
DCC-2036 also inhibits the SRC family kinases SRC, LYN, FGR, and HCK, and the receptor TKs KDR, FLT3, and TIE2 (IC50s=2-40 nM), but spares c-KIT (IC50=480 nM).
DCC-2036 potently inhibits unphosphorylated and phosphorylated of ABL1 native with IC50 of 0.75 and 2 nM, potently inhibits unphosphorylated and phosphorylated of ABL1 T315I with IC50 of 5 and 4 nM, also potently inhibits ABL1 H396P (IC50=1.4 nM).
DCC-2036 inhibits cellular proliferation of Ba/F3 cells expressing native or T315I mutant with IC50 of 5.4 and 13 nM, also inhibits proliferation of several common TKI-resistant mutants of BCR-ABL1, including G250E, Q252H, Y235F, E255K, V299L, F317L, and M351T with IC50 of 6-150 nM.
DCC-2036 prolongs survival in mouse Ba/F3 cell allograft models.
| M.Wt | 553.5869 | |
| Formula | C30H28FN7O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-Pyridinecarboxamide, 4-[4-[[[[3-(1,1-dimethylethyl)-1-(6-quinolinyl)-1H-pyrazol-5-yl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl- |
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1. Chan WW, et al. Cancer Cell. 2011 Apr 12;19(4):556-68.
2. Eide CA, et al. Cancer Res. 2011 May 1;71(9):3189-95.
3. O'Hare T, et al. Blood. 2011 Nov 10;118(19):5250-4.
4. O'Hare T, et al. Clin Cancer Res. 2011 Jan 15;17(2):212-21.
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