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Agerafenib hydrochloride

Catalog No. T14928   CAS 1227678-26-3
Synonyms: CEP-32496 (hydrochloride), RXDX-105 hydrochloride

Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).

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Agerafenib hydrochloride, CAS 1227678-26-3
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Rowbottom MW, et al. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

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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