CC-90003
- Product Name
- CC-90003
- CAS No.
- 1621999-82-3
- Chemical Name
- CC-90003
- Synonyms
- CC-90003;CC-90003 (CC90003);CC-90003, 10 mM in DMSO;Inhibitor,Extracellular signal regulated kinases,ERK,inhibit,CC90003,CC 90003,CC-90003;N-(2-((2-((2-Methoxy-5-methylpyridin-4-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-5-methylph;N-(2-((2-((2-Methoxy-5-methylpyridin-4-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-5-methylphenyl)acrylamide;2-Propenamide, N-[2-[[2-[(2-methoxy-5-methyl-4-pyridinyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]-5-methylphenyl]-
- CBNumber
- CB23165061
- Molecular Formula
- C22H21F3N6O2
- Formula Weight
- 458.44
- MOL File
- 1621999-82-3.mol
CC-90003 Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 125 mg/mL (272.66 mM);Water : < 0.1 mg/mL (insoluble)
- form
- Solid
- color
- White to off-white
Safety
- HS Code
- 2933998090
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0046792
- Product name
- CC-90003
- Purity
- 99.84%
- Packaging
- 5mg
- Price
- $140
- Updated
- 2021/12/16
- Product number
- BISN0236
- Product name
- N-(2-((2-((2-Methoxy-5-methylpyridin-4-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-5-methylphenyl)acrylamide
- Packaging
- 5mg
- Price
- $189
- Updated
- 2021/12/16
- Product number
- CS-0046792
- Product name
- CC-90003
- Purity
- 99.84%
- Packaging
- 10mg
- Price
- $240
- Updated
- 2021/12/16
- Product number
- CS-0046792
- Product name
- CC-90003
- Purity
- 99.84%
- Packaging
- 25mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- CS-0046792
- Product name
- CC-90003
- Purity
- 99.84%
- Packaging
- 50mg
- Price
- $740
- Updated
- 2021/12/16
CC-90003 Chemical Properties,Usage,Production
Uses
CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
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 () |
IC 50
ERK1; ERK2
References
[1] Monica M. Mita, et al. A phase Ia study of CC-90003, a selective extracellular signal-regulated kinase (ERK) inhibitor, in patients with relapsed or refractory BRAF or RAS-mutant tumors. Journal of Clinical Oncology 35, no. 15_suppl (May 20 2017) 2577-257
CC-90003 Preparation Products And Raw materials
Raw materials
Preparation Products
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