2-Propenamide, N-[2-[[2-[(2-methoxy-5-methyl-4-pyridinyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]-5-methylphenyl]-
CC-90003
CAS: 1621999-82-3
Molecular Formula: C22H21F3N6O2
2-Propenamide, N-[2-[[2-[(2-methoxy-5-methyl-4-pyridinyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]-5-methylphenyl]- - Names and Identifiers
| Name | CC-90003 |
| Synonyms | CC-90003 2-Propenamide, N-[2-[[2-[(2-methoxy-5-methyl-4-pyridinyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]-5-methylphenyl]- |
| CAS | 1621999-82-3 |
2-Propenamide, N-[2-[[2-[(2-methoxy-5-methyl-4-pyridinyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]-5-methylphenyl]- - Physico-chemical Properties
| Molecular Formula | C22H21F3N6O2 |
| Molar Mass | 458.44 |
| Storage Condition | Room Temprature |
| In vitro study | In the biochemical tests, cell experiments and mass spectrometry of 347 kinases, CC-90003 strongly inhibited the kinase activity of ERK1 and ERK2, and IC50 had good kinase selectivity at 10-20 nM. In the kinase library containing 258 kinases, CC-90003 inhibited 213 of them by less than 50%, it has moderate inhibitory activity on 28 kinases (50%-80% inhibition) and significant inhibitory effect on 17 kinases (>80%). Kinase screening in A375 cells, a melanoma cell line with the BRAF V600E mutation, showed only five kinases out of 194 (ERK1, ERK2, MKK4, MKK6 and FAK) was significantly inhibited (>80%) by 1 mM CC-90003. The same concentration had no significant inhibitory activity on 40 non-kinase enzymes and receptors (<14%). By iterative analysis, in cells, except ERK1/2, only three kinases were CC-90003 inhibited at biologically relevant concentrations: KDR, FLT3, and PDGFRa. Tumor cells with the BRAF mutation are particularly sensitive to CC-90003. In most (but not all) cases, CC-90003 has toxic effects on PDAC, lung and colon cancer cell lines with KRAS mutations. CC-90003 did not significantly inhibit the proliferation of normal lung fibroblasts or airway epithelial cells. |
| In vivo study | In the HCT-116 graft tumor in vivo model, within a certain range (12.5 mg B. I. d.-100 mg qd)CC-90003 well tolerated, while 50 mpk B. I. d. And 75 mpk B. I. d. Death of the animals was caused at 6-18 days of dosing. Both once-a-day and twice-a-day dosing frequencies resulted in inhibition of tumor growth. In the three KRAS mutant human xenograft models tested, CC-90003 all had anti-tumor activity. |
2-Propenamide, N-[2-[[2-[(2-methoxy-5-methyl-4-pyridinyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]-5-methylphenyl]- - References
| biological activity | CC-90003 is an irreversible inhibitor of ERK1/2 with IC50 of 10-20 nM, it has good kinase selectivity. |
| Target | Value |
Last Update：2024-04-10 22:29:15
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CAS: 1621999-82-3
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CAS: 1621999-82-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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