CC-90003
- CAS No.
- 1621999-82-3
- Chemical Name:
- CC-90003
- Synonyms
- CC-90003;Inhibitor,Extracellular signal regulated kinases,ERK,inhibit,CC90003,CC 90003,CC-90003;2-Propenamide, N-[2-[[2-[(2-methoxy-5-methyl-4-pyridinyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]-5-methylphenyl]-
- CBNumber:
- CB23165061
- Molecular Formula:
- C22H21F3N6O2
- Molecular Weight:
- 458.44
- MDL Number:
- MFCD31692404
- MOL File:
- 1621999-82-3.mol
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H302-H315-H319-H335 |
Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
HS Code | 2933998090 |
CC-90003 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0046792 | CC-90003 99.84% | 1621999-82-3 | 5mg | $140 | 2021-12-16 | Buy |
Apolloscientific | BISN0236 | N-(2-((2-((2-Methoxy-5-methylpyridin-4-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-5-methylphenyl)acrylamide | 1621999-82-3 | 5mg | $189 | 2021-12-16 | Buy |
ChemScene | CS-0046792 | CC-90003 99.84% | 1621999-82-3 | 10mg | $240 | 2021-12-16 | Buy |
ChemScene | CS-0046792 | CC-90003 99.84% | 1621999-82-3 | 25mg | $450 | 2021-12-16 | Buy |
ChemScene | CS-0046792 | CC-90003 99.84% | 1621999-82-3 | 50mg | $740 | 2021-12-16 | Buy |
CC-90003 Chemical Properties,Uses,Production
Biological Activity
CC-90003 is an irreversible inhibitor of ERK1/2 with IC50 of 10-20 nM and good kinase selectivity.
in vitro
CC-90003 potently inhibited the kinase activities of ERK1 and ERK2 in biochemical assays, cellular assays and mass spectrometry analysis of 347 kinases with IC50 at 10-20 nM quality, with Good kinase selectivity. In a kinase library containing 258 kinases, it has less than 50% inhibition on 213 kinases, moderate inhibitory activity (50%-80% inhibition) on 28 kinases, and significant inhibitory activity on 17 kinases Inhibition (>80%). Kinase screen in melanoma cell line A375 cells with BRAF V600E mutation, only 5 of 194 kinases (ERK1, ERK2, MKK4, MKK6 and FAK) were significantly inhibited (>80%) by 1 mM CC-90003 . However, the same concentration had no significant inhibitory activity (<14%) on 40 non-kinase enzymes and receptors. By iterative analysis, in cells, in addition to ERK1/2, only three kinases were inhibited by it at biologically relevant concentrations: KDR, FLT3 and PDGFRa. Tumor cells with BRAF mutations are particularly sensitive to it. In most, but not all, cases, it was toxic to KRAS-mutated PDAC, lung and colon cancer cell lines. It did not significantly inhibit the proliferation of normal lung fibroblasts or airway epithelial cells.
in vivo
In the HCT-116 xenograft in vivo model, CC-90003 was well tolerated within a range (12.5 mg bid-100 mg qd), while 50 mpk bid and 75 mpk bid induced elicited in animals on days 6-18 of dosing die. Both once-daily and twice-daily dosing frequencies resulted in inhibition of tumor growth. It has antitumor activity in all three KRAS-mutated human xenograft models tested.
target
Target | Value |
ERK1 () | |
ERK2 () |
CC-90003 Preparation Products And Raw materials
Raw materials
Preparation Products
CC-90003 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Shanghai XingMo Biotechnology Co., Ltd. | 13524779951 | 2075692521@qq.com | China | 310 | 55 |
BOC Sciences | 16314854226 | info@bocsci.com | United States | 9926 | 65 |
Beijing Solarbio Science & Tecnology Co., Ltd. | 010-50973130 4009686088 | 3193328036@qq.com | China | 29795 | 68 |
Twochem Co.Ltd. | 021-58111628 15800915896 | sales@twochem.com | China | 1789 | 58 |
Tianjin Kaifu Pharmaceutical Technology Co., Ltd. | 18081075745 | chemflowtech@sina.com | China | 1886 | 58 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |