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| 品牌 | absin | CAS | 1228591-30-7 |
|---|---|---|---|
| 分子式 | C27H18F4N4O3S | 纯度 | ＞98% |
| 分子量 | 554.52 | 货号 | abs810569 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a selective pan-RAF kinase inhibitor | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
TAK-632 1228591-30-7
| 产品描述 | |
| 描述 | TAK-632 is a selective pan-RAF kinase inhibitor with IC50 values of 2.4/1.4 nM for BRAF V600E/c-RAF; > 60 fold selectivity over VEGFR. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | TAK 632; TAK632 |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO 100 mg/mL (180.33 mM) Ethanol 2 mg/mL (3.6 mM) |
| 生物活性 | |
| 靶点 | C-Raf ,B-Raf ,Aurora B ,PDGFRβ ,FGFR3 |
| In vitro(体外研究) | TAK-632 inhibits phosphorylation of MEK and ERK in melanoma A375 cells (BRAFV600E) with IC50 of 12 nM and 16 nM, respectively. In human melanoma HMVII cells (NRASQ61K/BRAFG469V), TAK-632 also shows strong inhibition of pMEK and pERK with IC50 of 49 nM and 50 nM, respectively. Moreover, TAK-632 also exhibits antiproliferative activity in both A375 and HMVII cells with GI50 of 66 nM and 200 nM, respectively. TAK-632 induces RAF dimerization but inhibits the kinase activity of the RAF dimer because of its slow dissociation from RAF. The combination of TAK-632 and TAK-733 exhibits synergistic antiproliferative effects in BRAF- and NRAS-mutated melanoma cells. |
| In vivo(体内研究) | TAK-632 shows superior oral bioavailability in both rats and dogs. TAK-632 (3.9–24.1 mg/kg, p.o.) exhibits dose-dependent antitumor efficacy without severe body weight reduction in a melanoma A375 (BRAFV600E) xenograft model and a human melanoma HMVII (NRASQ61K/BRAFG469V) xenograft in rats. In NRAS-mutant melanoma SK-MEL-2 xenograft model, TAK-632 (60 or 120 mg/kg, p.o.) also exhibits potent antitumor efficacy without severe toxicity. |
| 研究领域 | |
| 研究领域 | CancerTumor biomarkers Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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