TAK733
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- CAS号:
- 1035555-63-5
- 英文名:
- TAK-733
- 英文别名:
- CS-547;TAK-733;TAK-733/TAK733;TAK-733 USP/EP/BP;(R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrim;3-[(2r)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione;(R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione;Pyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione, 3-[(2R)-2,3-dihydroxypropyl]-6-fluoro-5-[(2-fluoro-4-iodophenyl)amino]-8-methyl-;(R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione TAK 733
- 中文名:
- TAK733
- 中文别名:
- MEK变构抑制剂(TAK-733)
- CBNumber:
- CB42561497
- 分子式:
- C17H15F2IN4O4
- 分子量:
- 504.23
- MOL File:
- 1035555-63-5.mol
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TAK733化学性质
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沸点:
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530.5±60.0 °C(Predicted)
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密度:
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1.91±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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≥25.2 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
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形态:
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solid
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酸度系数(pKa):
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13.72±0.20(Predicted)
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TAK733性质、用途与生产工艺
TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1， AKT3， c-RAF， CamK1， CDK2及c-Met等活性。Phase 1。
TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells.
TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. TAK-733 is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans. TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg.
TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1， AKT3， c-RAF， CamK1， CDK2及c-Met等活性。Phase 1。
| Target | Value |
MEK1
(Cell-free assay)
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3.2 nM
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TAK-733是高度有效的选择性MEK变构位点抑制剂，IC50 为3.2 nM。TAK-733表现出有效的酶和细胞活性，对细胞中ERK磷酸化作用的EC50为1.9 nM。
TAK-733在人体肿瘤，包括黑色素瘤，结肠直肠癌，NSCLC，胰腺癌和乳腺癌的小鼠异种移植物模型中表现出广谱抗肿瘤活性。TAK-733具有良好的药代动力学和药效动力学耐受性，对于人类可每天一次口服给药。 TAK-733的最大有效剂量为10 mg/kg，每天一次。
TAK733
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-13449 | TAK733
TAK-733 | 1035555-63-5 | 2mg | 834元 |
| 2024/01/25 | HY-13449 | TAK733
TAK-733 | 1035555-63-5 | 5mg | 1252元 |
1035555-63-5, TAK733 相关搜索:
- MAPK
- Inhibitors
- 药靶配体
- 合成有机化合物配体
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- C17H15F2IN4O4
- MEK变构抑制剂(TAK-733)
- 1035555-63-5
- TAK-733 USP/EP/BP
- Pyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione, 3-[(2R)-2,3-dihydroxypropyl]-6-fluoro-5-[(2-fluoro-4-iodophenyl)amino]-8-methyl-
- 3-[(2r)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione
- CS-547
- (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrim
- (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione TAK 733
- (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione
- TAK-733/TAK733
- TAK-733