Belvarafenib (GDC5573, HM95573, RG6185) is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively. Belvarafenib also shows high inhibitory activity for FMS, DDR1 and DDR2 kinases, with IC50s of 10 nM, 23 nM and 44 nM, respectively.
| Molecular Weight | 478.93 |
| Formula | C23H16ClFN6OS |
| CAS Number | 1446113-23-0 |
| Solubility (25°C) | DMSO 12 mg/mL |
| Storage | 4°C, sealed |
| 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.
[4] No authors listed. Cancer Discov. ARAF Mutations Limit Response to RAF Dimer Inhibition
| Related Raf Products |
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Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM. |
| R18
R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. |
| PROTAC RAF degrader 1
PROTAC RAF degrader 1 is a PROTAC RAF degrader. |
| B-Raf IN 15
B-Raf IN 15 is a BRAF inhibitor. |
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