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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | Backorder |
Description | Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM). |
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. |
Alias | RXDX-105 hydrochloride, CEP-32496 (hydrochloride) |
Molecular Weight | 553.92 |
Formula | C24H23ClF3N5O5 |
Cas No. | 1227678-26-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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