| Identification | Back Directory | [Name]
1-Pyrrolidinecarboxamide, N-[3-[2-[[(1R)-2-hydroxy-1-methylethyl]amino]-6-(4-morpholinyl)-4-pyridinyl]-4-methylphenyl]-3-(2,2,2-trifluoroethyl)-, (3S)- | [CAS]
2639957-39-2 | [Synonyms]
exarafenib
1-Pyrrolidinecarboxamide, N-[3-[2-[[(1R)-2-hydroxy-1-methylethyl]amino]-6-(4-morpholinyl)-4-pyridinyl]-4-methylphenyl]-3-(2,2,2-trifluoroethyl)-, (3S)- | [Molecular Formula]
C26H34F3N5O3 | [MOL File]
2639957-39-2.mol | [Molecular Weight]
521.58 |
| Chemical Properties | Back Directory | [Boiling point ]
732.5±60.0 °C(Predicted) | [density ]
1.301±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, away from moisture and light | [form ]
Solid | [pka]
12.59±0.70(Predicted) | [color ]
Light yellow to green yellow | [InChIKey]
GZMYLSJUNSCMTD-MOPGFXCFSA-N | [SMILES]
N1(C(NC2=CC=C(C)C(C3C=C(N4CCOCC4)N=C(N[C@H](C)CO)C=3)=C2)=O)CC[C@@H](CC(F)(F)F)C1 |
| Hazard Information | Back Directory | [Uses]
Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity[1][2]. | [in vivo]
Exarafenib (RAF/KIN_2787; 3-30 mg/kg; Orally; twice daily; 29 days) is effective against BRAFmut & NRASmut human melanoma xenografts in vivo[1]. | Animal Model: | BALB/c nude mice xenograft models of BRAF and NRAS-mutant melanoma[1] | | Dosage: | 3, 5, 10, 20, 30 mg/kg | | Administration: | Orally; twice daily (BID); 29 days | | Result: | Was effective against BRAFmut & NRASmut human melanoma xenografts in vivo.
|
| [IC 50]
RAF; p38 MAPK | [storage]
4°C, away from moisture and light | [References]
[1] Miller N, et, al. Antitumor activity of KIN-2787, a next-generation pan-RAF inhibitor, in combination with MEK inhibition in preclinical models of human NRAS mutant melanoma.2022 Jun 2;40(16): e15099.
[2] WHO Drug Information. International Nonproprietary Names for Pharmaceutical |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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