LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively.
| Molecular Weight | 424.51 |
| CAS Number | 1454682-72-4 |
| Solubility (25°C) | DMSO ≥ 38 mg/mL |
| 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.
[5] Robert Roskoski Jr. Targeting oncogenic Raf protein-serine/threonine kinases in human cancers
| Related Raf Products |
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| Cyclorasin 9A5
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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Raf inhibitor 3 is a Raf inhibitor. |
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