BMS-986165
BMS-986165是具有选择性、强效、变构抑制剂的酪氨酸激酶2 (Tyk2)。
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | BMS-986165 |
|---|---|
| Iupac 化学名称 | 6-(Cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1h-1,2,4-triazol-3-yl)phenyl)amino)-n-(methyl-d3)pyridazine-3-carboxamide |
| 同义词 | BMS-986165 ; BMS 986165 ; BMS986165 ; |
| 英文同义词 | BMS-986165 ; BMS 986165 ; BMS986165 ; |
| 分子式 | C20H22N8O3 |
| 分子量 | 425.46 |
| Smile | C1(CC1)C(=O)NC1=CC(=C(N=N1)C(=O)NC([2H])([2H])[2H])NC1=C(C(=CC=C1)C1=NN(C=N1)C)OC |
| InChiKey | BZZKEPGENYLQSC-FIBGUPNXSA-N |
| InChi | InChI=1S/C20H22N8O3/c1-21-20(30)16-14(9-15(25-26-16)24-19(29)11-7-8-11)23-13-6-4-5-12(17(13)31-3)18-22-10-28(2)27-18/h4-6,9-11H,7-8H2,1-3H3,(H,21,30)(H2,23,24,25,29)/i1D3 |
| Cas号 | 1609392-27-9 |
| 相关CAS号 | 1609392-27-9 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色至白色固体 |
|---|---|
| 纯度 | >99% |
| 存储 | 短期可在0-4度保存，数天至数月；长期可在-20度保存三年。 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 可在常温下运输 |
| 海关编码 |
| Targets | TYK2 inhibitor |
|---|---|
| Mechanism | BMS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM). BMS-986165 potently inhibited IL-23-, IL-12-, and Type I interferon-driven cellular signaling and transcriptional responses (IC50 range 2-14 nM). BMS-986165 was approximately 200-fold selective against JAK1/3-dependent signaling in IL-2-stimulated T cells and >3,000-fold selective over JAK2-dependent EPO-induced signaling in TF-1 cells. |
| Cell study | |
| Animal study | |
| Clinical study |
1: Papp K, Gordon K, Thaçi D, Morita A, Gooderham M, Foley P, Girgis IG, Kundu S, Banerjee S. Phase 2 Trial of Selective Tyrosine Kinase 2 Inhibition in Psoriasis. N Engl J Med. 2018 Oct 4;379(14):1313-1321. doi: 10.1056/NEJMoa1806382. Epub 2018 Sep 11. PubMed PMID: 30205746.
2. Gillooly K, Zhang Y, Yang X, Zupa-Fernandez A, Cheng L, Strnad J, Cunningham M, Heimrich E, Zhou X, Chen J, Chaudhry C, Li S, McIntyre K, Carman J, Moslin R, Wrobleski S, Weinstein D, Burke J. BMS-986165 Is a Highly Potent and Selective Allosteric Inhibitor of Tyk2, Blocks IL-12, IL-23 and Type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Systemic Lupus Erythematosus and Inflammatory Bowel Disease [abstract]. Arthritis Rheumatol. 2016; 68 (suppl 10). https://acrabstracts.org/abstract/bms-986165-is-a-highly-potent-and-selective-allosteric-inhibitor-of-tyk2-blocks-il-12-il-23-and-type-i-interferon-signaling-and-provides-for-robust-efficacy-in-preclinical-models-of-systemic-lupus-e/. Accessed November 7, 2018.
