Bulk Inquiry
Rebastinib
- DCC-2036 - D 1919
Axon 2123
CAS:
1020172-07-9
Purity:
99%
- Soluble in DMSO
- MF: C30H28FN7O3
- MW: 553.59
Description
An orally active Bcr-ABL inhibitor; being a ABL Switch-control inhibitor that potently inhibits BCR-ABL1 gatekeeper mutant T315I (IC50: 0.8 nM for native ABL1 and 4 nM in a ABL1T3151 kinase assay). DCC-2036 has efficacy in a mouse model of T315I-induced CML and against cells of patients with CML. In addition, DCC-2036 also inhibited the SRC family kinases SRC, LYN, FGR, and HCK, and the receptor TKs KDR, FLT3, and TIE2, but not c-KIT (IC50 of 34 nM, 29 nM, 38 nM, 40 nM, 4 nM, 2 nM, 6 nM, and 481 nM respectively)
More Information
| Parent CAS No. | 1020172-07-9 |
|---|---|
| Chemical Name | 4-(4-(3-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)ureido)-3-fluorophenoxy)-N-methylpicolinamide |
| SMILES | C1C=C2C=C(N3N=C(C(C)(C)C)C=C3NC(=O)NC3C(F)=CC(OC4C=CN=C(C(=O)NC)C=4)=CC=3)C=CC2=NC=1 |
| MFCD | MFCD19443646 |
| InChi | InChI=1S/C30H28FN7O3/c1-30(2,3)26-17-27(38(37-26)19-7-9-23-18(14-19)6-5-12-33-23)36-29(40)35-24-10-8-20(15-22(24)31)41-21-11-13-34-25(16-21)28(39)32-4/h5-17H,1-4H3,(H,32,39)(H2,35,36,40) |
| InChiKey | WVXNSAVVKYZVOE-UHFFFAOYSA-N |
| CID | 25066467 |
| Short Description | Bcr-Abl inhibitor |
References
- WW Chan et al. Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036. Cancer Cell 2011, 19(4), 556–568.
- CA Eide 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, 71(9), 3189-95.
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 1137 | PD180970 |
From $143.00 |
| 1392 | Dasatinib |
From $99.00 |
| 1394 | Imatinib mesylate |
From $66.00 |
| 1396 | Nilotinib |
From $55.00 |
| 1407 | SKI 606 |
From $82.50 |
| 1857 | AP 24534 |
From $77.00 |
| 1882 | GNF 2 |
From $121.00 |
| 2121 | INNO 406 |
From $93.50 |
| 2219 | AT 9283 |
From $99.00 |
| 2757 | Asciminib |
From $132.00 |
| 3168 | Nilotinib hydrochloride |
From $77.00 |
Other Categories
Get a Quote for
Loading...