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Vemurafenib (PLX4032; RG7204; RO5185426) is a first-in-class selective B-RAF inhibitor that inhibits the activity of RAFV600E and c-RAF-1 with IC50 at 31 nM and 48 nM, respectively.
| Molecular Weight | 494.95 |
| Formula | C23H13D5ClF2N3O3S |
| CAS Number | 1365986-90-8 |
| Solubility (25°C) | N/A |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| Exarafenib
Exarafenib (KIN-2787) is a highly selective, potent, next-generation, pan-RAF inhibitor with activity across BRAF and RAS mutant human tumor cell models. Exarafenib has anticancer activity by suppression of downstream MAPK pathway signaling. |
| Tinlorafenib
Tinlorafenib (PF-07284890) is an orally active BRAF kinase inhibitor, with IC50 values of 4.25 and 2.7 nM for BRAFV600E/V600K respectively. |
| Vemurafenib-d7
Vemurafenib (PLX4032; RG7204; RO5185426) is a first-in-class selective B-RAF inhibitor that inhibits the activity of RAFV600E and c-RAF-1 with IC50 at 31 nM and 48 nM, respectively. Vemurafenib can induce autophagy. |
| LUT014
LUT014, a B-Raf inhibitor with an IC50 value of 11.7 nM, was developed for the study of reducing acne-like lesions associated with EGFR inhibitors at restricted doses. |
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GNE-9815 is one of the most selective kinase inhibitors of RAF, targeting KRAS mutant cancers by combination of drugs. |
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