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Agerafenib hydrochloride

Catalog No. T14928 CAS 1227678-26-3

Synonyms: RXDX-105 hydrochloride, CEP-32496 (hydrochloride)

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

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Agerafenib hydrochloride Chemical Structure

Agerafenib hydrochloride, CAS 1227678-26-3

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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	BRAF:36 nM （kd）, B-Raf (V600E):14 nM （kd）, c-Kit:2 nM （kd）, JAK2:4700 nM （kd）, Raf:39 nM （kd）, EGFR:22 nM （kd）, VEGFR2:8 nM （kd）, MEK2:8300 nM （kd）, EphA2:14 nM （kd）, CSF1R:9 nM （kd）, Abl-1:3 nM （kd）, MEK1:7100 nM （kd）, Lck:2 nM （kd）, RET:2 nM （kd）, c-Met:513 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	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

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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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.

Keywords

Agerafenib hydrochloride 1227678-26-3 Apoptosis Tyrosine Kinase/Adaptors c-RET c-Kit RXDX105 Hydrochloride CEP 32496 CEP-32496 RXDX-105 hydrochloride RXDX 105 Hydrochloride CEP32496 RXDX-105 Hydrochloride Agerafenib Hydrochloride CEP-32496 (hydrochloride) inhibitor inhibit

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