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LY3200882 是一种高度选择性的、口服活性的、具有 ATP 竞争性的 TGF-β 受体 1 型 (ALK5) 抑制剂(IC50:38.2 nM)。它能够抑制多种促肿瘤活性,可用作免疫调节剂。
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LY3200882 是一种高度选择性的、口服活性的、具有 ATP 竞争性的 TGF-β 受体 1 型 (ALK5) 抑制剂(IC50:38.2 nM)。它能够抑制多种促肿瘤活性,可用作免疫调节剂。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 397 | 现货 | |
5 mg | ¥ 993 | 现货 | |
10 mg | ¥ 1,570 | 现货 | |
25 mg | ¥ 2,670 | 现货 | |
50 mg | ¥ 3,730 | 现货 | |
100 mg | ¥ 5,320 | 现货 | |
500 mg | ¥ 10,800 | 现货 |
产品描述 | LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). |
靶点活性 | TGFβRI:38.2 nM (IC50) |
体外活性 | LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells. LY3200882 has shown anti-metastatic activity in vitro in migration assays. In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed na?ve T cell activity and restore proliferation [1]. |
体内活性 | LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose-dependent fashion. LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer) [1]. |
分子量 | 435.52 |
分子式 | C24H29N5O3 |
CAS No. | 1898283-02-7 |
Smiles | CC(C)(O)c1cc(Nc2cc(Oc3cn(nc3C3CCOCC3)C3CC3)ccn2)ccn1 |
密度 | 1.36 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 4.36 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
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