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目錄:MedChemExpress LLC>>生化試劑>> Agerafenib | MCE

Agerafenib | MCE
  • Agerafenib | MCE
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更新時(shí)間:2023-06-27 09:31:22瀏覽次數(shù):202評價(jià)

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CAS 1188910-76-0 純度 99.63%
分子量 517.46 分子式 C??H??F?N?O?
供貨周期 現(xiàn)貨 規(guī)格 5 mg
貨號 HY-15200 應(yīng)用領(lǐng)域 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥
Agerafenib | MCEAgerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of <b>BRAF<sup>V600E</sup></b> with a <b>K<sub>d</sub></b> of 14 nM.

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Agerafenib

CAS No. : 1188910-76-0

產(chǎn)品活性:Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.

研究領(lǐng)域:MAPK/ERK Pathway

作用靶點(diǎn):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 versus CYP2C19.

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).

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