购物车
- 全部删除
- 您的购物车当前为空
SAR405838 (MI 773) 是 MI-773 的类似物,具有抗肿瘤活性。它是一种高效、选择性的MDM2-p53相互作用抑制剂,与 MDM2 结合的Ki 值为 0.88 nM。
SAR405838 (MI 773) 是 MI-773 的类似物,具有抗肿瘤活性。它是一种高效、选择性的MDM2-p53相互作用抑制剂,与 MDM2 结合的Ki 值为 0.88 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 496 | 现货 | |
5 mg | ¥ 1,230 | 现货 | |
10 mg | ¥ 1,980 | 现货 | |
25 mg | ¥ 3,590 | 现货 | |
50 mg | ¥ 5,190 | 现货 | |
100 mg | ¥ 7,220 | 现货 | |
200 mg | ¥ 9,730 | 现货 |
产品描述 | MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1. |
靶点活性 | MDM2:0.88 nM(Ki) |
体外活性 | SAR405838与MDM2结合,Ki值为0.88 nM。在包括SJSA-1(IC50, 0.092 μM)、RS4;11(IC50, 0.089 μM)、LNCaP(IC50, 0.27 μM)和HCT-116(IC50, 0.20 μM)在内的癌症细胞系中,SAR405838显著抑制细胞增长,并且对于具有突变或删除的p53基因的癌症细胞系,如SAOS-2(IC50, >10 μM)、PC-3(IC50, >10 μM)、SW620(IC50, >10 μM)和HCT-116(p53-/-)(IC50, >20 μM)细胞,显示出高度选择性。[1] |
体内活性 | 在SJSA-1骨肉瘤、急性淋巴细胞白血病RS4;11、LNCaP前列腺癌和HCT-116结肠癌异种移植模型中,SAR405838 (p.o.) 通过剂量依赖性方式有效抑制肿瘤生长,具体剂量包括10 mg/kg、30 mg/kg、50 mg/kg、100 mg/kg以及200 mg/kg。[1] |
激酶实验 | Fluorescence-polarization binding assay: Binding af?nities of MDM2 inhibitors and p53 peptide to MDM2 protein are determined using an Fluorescence-polarization (FP) binding assay. Binding af?nities of MI-773 to Bcl-2, Bcl-xL, Mcl-1, and β-catenin are determined using a competitive FP-based assay, and its binding af?nity to MDMx is determined using Biolayer Interferometry technology. |
细胞实验 | Cell growth inhibition activity is determined in a water-soluble tetrazolium-based assay. Cell death is measured by trypan blue staining and apoptosis is determined using an Annexin V-FLUOS staining kit.(Only for Reference) |
别名 | MI-77301, MI-773, MI773, MI 773 |
分子量 | 562.5 |
分子式 | C29H34Cl2FN3O3 |
CAS No. | 1303607-60-4 |
Smiles | CC(C)(C)C[C@@H]1N[C@H]([C@H](c2cccc(Cl)c2F)[C@]11C(=O)Nc2cc(Cl)ccc12)C(=O)N[C@H]1CC[C@H](O)CC1 |
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: 93 mg/mL (165.33 mM), Sonication is recommended. Ethanol: 29 mg/mL (51.56 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
|
评论内容