| Identification | Back Directory | [Name]
N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(methylcarbamoyl)pyridin-4-yl)oxy]phenyl]urea | [CAS]
1020172-07-9 | [Synonyms]
CS-1867
Rebastinib
DCC2036;DCC 2036
Rebastinib Tosylate
Rebastinib(DCC-2036)
DCC-2036 (Rebastinib)
DCC2036; DCC-2036; DCC 2036; REBASTINIB.
4-(4-(3-(3-(tert-Butyl)-1-(quinolin-6-yl)-1H-pyrazol-5-yl)ureido)-3-fluorophenoxy)-N-methylpic
N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(MethylcarbaMoyl)pyridin-4-yl)
4-(4-(3-(3-(tert-Butyl)-1-(quinolin-6-yl)-1H-pyrazol-5-yl)ureido)-3-fluorophenoxy)-N-methylpicolinamide
4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea
N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(methylcarbamoyl)pyridin-4-yl)oxy]phenyl]urea
N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(methylcarbamoyl)pyridin-4-yl)oxy]phenyl]urea USP/EP/BP
2-Pyridinecarboxamide, 4-[4-[[[[3-(1,1-dimethylethyl)-1-(6-quinolinyl)-1H-pyrazol-5-yl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-
N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(methylcarbamoyl)pyridin-4-yl)oxy]phenyl]urea DCC-2036 (Rebastinib) | [Molecular Formula]
C30H28FN7O3 | [MDL Number]
MFCD19443646 | [MOL File]
1020172-07-9.mol | [Molecular Weight]
554 |
| Chemical Properties | Back Directory | [Melting point ]
>181°C (dec.) | [Boiling point ]
666.8±55.0 °C(Predicted) | [density ]
1.32 | [storage temp. ]
-20°C Freezer | [solubility ]
Methanol (Slightly) | [form ]
Solid | [pka]
12.25±0.70(Predicted) | [color ]
Off-White |
| Hazard Information | Back Directory | [Description]
Rebastinib is an orally bioavailable tyrosine kinase inhibitor that inhibits Abl1 (IC50 = 0.8 nM) as well as the gatekeeper mutant Abl1T315I (IC50 = 4 nM) and the activation loop mutant Abl1H396P.1 It also inhibits the Src family kinases Src, Lyn, Fgr, and Hck and the tyrosine kinases KDR, FLT3, and Tie2 at nanomolar concentrations. Rebastinib inhibits mutant Abl1T315I signaling and prolongs survival in a mouse Ba/F3 cell allograft model.1,2 Rebastinib also exhibits in vivo antineoplastic activity against cells with the T674I point mutation of FIP1-like-1-platelet-derived growth factor receptor α.3 | [Uses]
A conformational control inhibitor of Abl1 and Abl1-T315I with IC50s of 0.8 nM and 4 nM, respectively. | [Definition]
ChEBI: DCC-2036 is a member of the class of ureas that is urea in which one of the nitrogens bears a 3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl substituent, while the other bears a 2-fluoro-4-{[2-(methylcarbamoyl)pyridin-4-yl]oxy}phenyl substituent. It has a role as a tyrosine kinase inhibitor. It is a member of quinolines, a pyridinecarboxamide, a member of pyrazoles, an organofluorine compound and a member of phenylureas. | [References]
[1] chan w w, wise s c, kaufman m d, 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. |
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