Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).
Description | Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM). |
Targets&IC50 | CRAF:39 nM (kd), JAK-2:4700 nM (kd), EGFR:22 nM (kd), BRafV600E:14 nM (kd), c-Kit:2 nM (kd), BRAF:36 nM (kd), VEGFR-2:8 nM (kd), Abl-1:3 nM (kd), CSF-1R:9 nM (kd), EPHA2:14 nM (kd), MEK-2:8300 nM (kd), Lck:2 nM (kd), c-Met:513 nM (kd), RET:2 nM (kd), MEK-1:7100 nM (kd) |
In vitro | Agerafenib exhibits high potency against several BRAF V600E-dependent cell lines and selective cytotoxicity for tumor cell lines expressing mutant BRAF V600E. It shows potent binding (BRAF V600E, Kd: 14 nM) and cellular activity (pMEK IC50=82 nM and A375 proliferation IC50=78 nM), with activity in the proliferation assay. Agerafenib also exhibits a favorable CYP450 inhibition profile, with measured IC50 values greater than 10 μM versus the CYP1A2, CYP2C9, CYP2D6, and CYP3A4 isoforms and an IC50=3.4 μM versus CYP2C19. |
In vivo | Agerafenib exhibits an exceptional PK profile in mouse, dog, and cynomolgus monkey. Administration of Agerafenib to beagle dogs (single dose of 1 mg/kg i.v and 10 mg/kg p.o) results in low clearance (CL=5.0 (mL/min)/kg) and excellent bioavailability (%F=100). Similarly, in cynomolgus monkey, the administration of Agerafenib (single dose of 1 mg/kg i.v and 10 mg/kg p.o) leads to high oral exposure due to low clearance (CL=6.7 mL/min/kg) and excellent bioavailability (%F=100). Oral administration of Agerafenib to Colo-205 tumor xenograft-bearing mice results in significant inhibition of pMEK in tumor cell lysates. |
Synonyms | CEP-32496 (hydrochloride), RXDX-105 hydrochloride |
Molecular Weight | 553.92 |
Formula | C24H23ClF3N5O5 |
CAS No. | 1227678-26-3 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Agerafenib hydrochloride 1227678-26-3 蛋白酪氨酸激酶 凋亡 c-Kit c-RET CEP-32496 (hydrochloride) RXDX-105 hydrochloride Inhibitor inhibitor inhibit