| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| N646407-1mg |
1mg |
期货  |
| |
| N646407-5mg |
5mg |
期货 |
|
| 别名 | 努米达司他 |
|---|---|
| 英文别名 | CB1158, 2HCl | NUMIDARGISTAT [INN] | NUMIDARGISTAT [WHO-DD] | numidargistatum | CB 1158 | WHO 11086 | 2095732-06-0 | NSC803247 | NSC-803247 | Numidargistat | DB15286 | (3R,4S)-1-(L-alanyl)-3-amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid | (3R,4S)- |
| 规格或纯度 | ≥98% |
| 英文名称 | Numidargistat |
| 生化机理 | Numidargistat（CB-1158）是一种强效的精氨酸酶口服活性抑制剂，对重组人精氨酸酶 1 和重组人精氨酸酶 2 的 IC 50 s 分别为 86 nM 和 296 nM。免疫肿瘤学制剂。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 产品介绍 |
Numidargistat (CB-1158) is a potent and orally active inhibitor of arginase , with IC 50 s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2 , respectively. Immuno-oncology agent In Vitro Numidargistat is a potent and orally-bioavailable inhibitor of arginase, with IC 50 s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC 50 s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC 50 , 122 nM). Numidargistat also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC 50 s of 32, 139, 210 μM, respectively. Numidargistat show no effect on NOS. In addition, Numidargistat is not directly cytotoxic to murine cancer cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Numidargistat (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 86 nM (Arginase 1), 296 nM (Arginase 2) |
| 纯度 | ≥98% |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | (3R,4S)-3-amino-1-[(2S)-2-aminopropanoyl]-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid |
| INCHI | 1S/C11H22BN3O5/c1-7(13)9(16)15-5-8(3-2-4-12(19)20)11(14,6-15)10(17)18/h7-8,19-20H,2-6,13-14H2,1H3,(H,17,18)/t7-,8-,11-/m0/s1 |
| InChi Key | ZZJLMZYUGLJBSO-LAEOZQHASA-N |
| Smiles | B(CCCC1CN(CC1(C(=O)O)N)C(=O)C(C)N)(O)O |
| Isomeric SMILES | B(CCC[C@H]1CN(C[C@]1(C(=O)O)N)C(=O)[C@H](C)N)(O)O |
| 关联CAS | 2095732-06-0 |
| PubChem CID | 131801114 |
| MeSH Entry Terms | (3R,4S)-3-amino-1-((2S)-2-aminopropanoyl)-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid;CB-1158 |
| 分子量 | 287.12 |
| 分子量 | 287.120 g/mol |
|---|---|
| XLogP3 | |
| 氢键供体数Hydrogen Bond Donor Count | 5 |
| 氢键受体数Hydrogen Bond Acceptor Count | 7 |
| 可旋转键计数Rotatable Bond Count | 6 |
| 精确质量Exact Mass | 287.165 Da |
| 单同位素质量Monoisotopic Mass | 287.165 Da |
| 拓扑极表面积Topological Polar Surface Area | 150.000 Ų |
| 重原子数Heavy Atom Count | 20 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 381.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 3 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
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