BMS-986165
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.
BMS-986165, Bulk in stock,
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Chemical Information
| Name | BMS-986165 |
|---|---|
| Iupac Chemical Name | 6-(Cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1h-1,2,4-triazol-3-yl)phenyl)amino)-n-(methyl-d3)pyridazine-3-carboxamide |
| Synonyms | BMS-986165 ; BMS 986165 ; BMS986165 ; |
| Molecular Formula | C20H22N8O3 |
| Molecular Weight | 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 Number | 1609392-27-9 |
| Related CAS | 1609392-27-9 |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid to white solid |
|---|---|
| Purity | >99% |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature |
| HS Code |
| 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.
Chemical Structure
