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Trametinib is an inhibitor of MEK1 and -2. It inhibits B-RAF- and C-RAF-induced phosphorylation... more
Product information "Trametinib"
Trametinib is an inhibitor of MEK1 and -2. It inhibits B-RAF- and C-RAF-induced phosphorylation of MEK1 (IC50s = 3.4 and 1.8 nM, respectively) and MEK2 (IC50s = 1.6 and 0.92 nM, respectively). Trametinib inhibits the growth of two human colorectal cancer cell lines expressing mutant B-RAF (IC50s = 0.48 and 0.52 nM) and seven cell lines expressing mutant K-Ras (IC50s = 2.2-174 nM) but does not inhibit the growth of wild-type COLO 320DM cells expressing both B-RAF and K-Ras (IC50 = >10,000 nM). It reduces tumor growth in HT-29 and COLO 205 mouse xenograft models when used at doses of 0.3 and 1 mg/kg per day. Trametinib (0.03 and 0.1 mg/kg per day) also decreases M. tuberculosis-induced increases in hind paw volume in a rat model of arthritis. Formulations containing trametinib, in combination with dabrafenib, have been used in the treatment of metastatic mutant B-RAFV600E melanoma.Formal Name: N-[3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]-acetamide. CAS Number: 871700-17-3. Synonyms: GSK1120212, JTP-74057. Molecular Formula: C26H23FIN5O4. Formula Weight: 615.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 3 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 250, 330 nm. SMILES: CC(NC1=CC(N2C(C(C(N(C3CC3)C2=O)=O)=C(NC4=CC=C(I)C=C4F)N5C)=C(C)C5=O)=CC=C1)=O. InChi Code: InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34). InChi Key: LIRYPHYGHXZJBZ-UHFFFAOYSA-N.
Keywords: | GSK1120212, JTP-74057, N-[3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]-acetamide |
Supplier: | Cayman Chemical |
Supplier-Nr: | 16292 |
Properties
Application: | MEK1 / MEK2 inhibitor |
MW: | 615.4 D |
Formula: | C26H23FIN5O4 |
Purity: | >95% |
Format: | Crystalline Solid |
Database Information
CAS : | 871700-17-3| Matching products |
KEGG ID : | K04368 | Matching products |
Handling & Safety
Storage: | -20°C |
Shipping: | +20°C (International: -20°C) |
Signal Word: | Danger |
GHS Hazard Pictograms: |
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H Phrases: | H317, H361, H372 |
P Phrases: | P201, P202, P260, P261, P264, P270, P272, P280, P302+352, P308+313, P314, P321, P333+313, P362+364, P405, P501 |
Caution
Our products are for laboratory research use only: Not for administration to humans!
Our products are for laboratory research use only: Not for administration to humans!
Information about the product reference will follow.
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