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TAK-632

CAS No. : 1228591-30-7

MCE 国际站：TAK-632

产品活性：TAK-632 是一种有效的 pan-RAF 抑制剂，作用于 CRAF，BRAF^V600E 和 BRAF^WT，IC₅₀ 分别为 1.4，2.4 和 8.3 nM。

研究领域：MAPK/ERK Pathway  |  Epigenetics  |  Cell Cycle/DNA Damage

作用靶点：Raf  |  Aurora Kinase

In Vitro: TAK-632 inhibits PDGFRβ, FGFR3, GSK3β, CDK2, P38α, PDGFRα, TIE2, and CDK1 with a range of IC₅₀ values from 120-790 nM. CHK1, IKKβ, and MEK1 are inhibited over an IC₅₀ range of 1400-1700 nM. With 1 h of preincubation time, TAK-632 inhibits BRAF and CRAF in an ATP competitive manner (at low ATP concentrations BRAF IC₅₀: 15 nM; CRAF: 8.1 nM). The respective biochemical activity of TAK-632 against BRAF and CRAF reduces to IC₅₀ values of 58 nM and 62 nM at high ATP concentrations.TAK-632 demonstrates strong inhibition of pMEK and pERK in HMVII cells with IC₅₀ values of 49 nM and 50 nM, respectively. TAK-632 shows strong antiproliferative effects both in A375 and SK-MEL-2 cells (GI₅₀ of 40-190 nM in A375 cells and GI₅₀ of 190-250 nM in SK-MEL-2 cells).

In Vivo: TAK-632 demonstrates dramatically improved solubility (740 μg/mL) in pH 6.8 phosphate buffer and exhibits significant oral absorption (at a dose of 25 mg/kg, AUC, 32.47 μg h/mL; F, 51.7%) in rats. In a dog PK study, 10 mg/kg administration of TAK-632 also shows superior oral bioavailability (F: 108%).Oral single administration of TAK-632 inhibits pERK in tumors at 8 h after its administration over a dose range of 1.9-24.1 mg/kg. In particular, 9.7-24.1 mg/kg dosing with TAK-632 strongly inhibits pERK levels to 11% of the control. TAK-632 exhibits dose-dependent antitumor efficacy without severe body weight reduction over a dose range of 3.9-24.1 mg/kg. Significant tumor regression is observed at 9.7 mg/kg and 24.1 mg/kg (T/C=−2.1% and −12.1%, respectively). TAK-632 exhibits potent antitumor efficacy when orally administered at 60 mg/kg once daily (T/C=37%, P<0.001) or at 120 mg/kg once daily (T/C=29%, P<0.001) for 21 days without severe toxicity in NRAS-mutant melanoma using a SK-MEL-2 xenograft model.

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