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CAS No. : 1188910-76-0
MCE 国际站:Agerafenib
产品活性:Agerafenib (CEP-32496; RXDX-105) 是一种口服高效的 BRAFV600E 抑制剂,Kd 为 14 nM。
研究领域:MAPK/ERK Pathway
作用靶点:Raf
In Vitro: Agerafenib (CEP-32496) exhibits high potency against several BRAFV600E-dependent cell lines and selective cytotoxicity for tumor cell lines expressing mutant BRAFV600E versus those containing wild-type BRAF. Agerafenib exhibits potent binding (BRAFV600E 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.
In Vivo: Oral administration of Agerafenib (CEP-32496) to Colo-205 tumor xenograft-bearing mice results in significant inhibition of pMEK in tumor cell lysates. For instance, a single 30 mg/kg (po) dose of Agerafenib leads to a 50 and 75% inhibition of normalized pMEK in tumor lysates at the 2 and 6 h postdose time point, respectively (p<0.03), while a 55 mg/kg (po) dose resulted in a 75% to 57% (p<0.03) inhibition of pMEK at 2 through 10 h post administration, with normalization to baseline by 24 h. Agerafenib exhibits an exceptional PK profile in mouse, dog, and cynomolgus monkey. Administration of Agerafenib to beagle dogs (single dose of 1 mg/kg iv and 10 mg/kg po) 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 iv and 10 mg/kg po) leads to high oral exposure due to low clearance (CL=6.7 mL/min/kg) and excellent bioavailability (%F=100).
相关产品:Covalent Screening Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Covalent Screening Library | Oxygen Sensing Compound Library | Ferroptosis Compound Library | Orally Active Compound Library | Glutamine Metabolism Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Obesity Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | B-Raf IN 2 | Avutometinib | Sorafenib-d4 | AZ 628 | B-Raf IN 7 | Antitumor agent-60 | Sorafenib Tosylate | Dabrafenib Mesylate | SB-682330A | Belvarafenib TFA | L-779450 | B-Raf IN 9 | Debromohymenialdisine | Raf inhibitor 1 | TBAP-001 | RRD-251 | BI-882370 | Encorafenib-13C,d3 | PLX-4720 | TAK-632 | Norartocarpetin | Encorafenib | LUT014 | Rineterkib | Raf inhibitor 2 | Regorafenib monohydrate | AD57 | AD80
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