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

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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

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Safety

HS Code: 2933998090

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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.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0046792
Product name: CC-90003
Purity: 99.84%
Packaging: 5mg
Price: $140
Updated: 2021/12/16

Apolloscientific

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

ChemScene

Product number: CS-0046792
Product name: CC-90003
Purity: 99.84%
Packaging: 10mg
Price: $240
Updated: 2021/12/16

ChemScene

Product number: CS-0046792
Product name: CC-90003
Purity: 99.84%
Packaging: 25mg
Price: $450
Updated: 2021/12/16

ChemScene

Product number: CS-0046792
Product name: CC-90003
Purity: 99.84%
Packaging: 50mg
Price: $740
Updated: 2021/12/16

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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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CC-90003 Suppliers

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1621999-82-3, CC-90003Related Search:

CC-90003

2-Propenamide, N-[2-[[2-[(2-methoxy-5-methyl-4-pyridinyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]-5-methylphenyl]-

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-methylphenyl)acrylamide

CC-90003, 10 mM in DMSO

CC-90003 (CC90003)

N-(2-((2-((2-Methoxy-5-methylpyridin-4-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-5-methylph

1621999-82-3