BMS-986165
- CAS No.
- 1609392-27-9
- Chemical Name:
- BMS-986165
- Synonyms
- Deucravacitinib;6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl) phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide;Tyk2-IN-4;Deucravacitinb;BMS-986165 API;Deucravacitinib (TYK2-IN-4;Deucravacitinib(BMS986165);TYK2-IN-4;BMS986165;BMS-986165;BMS 986165;DeucravacitinibQ: What is Deucravacitinib Q: What is the CAS Number of Deucravacitinib;6-cyclopropaneamido-4-{[2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl]amino}-N-(2H?)methylpyridazine-3-carboxamide
- CBNumber:
- CB74808663
- Molecular Formula:
- C20H22N8O3
- Molecular Weight:
- 422.45
- MOL File:
- 1609392-27-9.mol
- Modify Date:
- 2024/7/3 13:03:20
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS08 |
|---|---|
| Signal word | Danger |
| Hazard statements | H361f-H372 |
| Precautionary statements | P260-P264-P270-P314-P501 |
BMS-986165 Chemical Properties,Uses,Production
General Description
Deucravacitinib, a highly selective allosteric TYK2 inhibitor, received its first approval from the FDA in 2022 for the treatment of adults with moderate-to-severe plaque psoriasis who are candidates for systemic therapy or phototherapy protein and lipid kinases and pseudokinases with the exception of BMPR2 (IC50 = 193 nM) and JAK1 JH2 pseudokinase domain (IC50 = 1 nM). Despite its potent affinity for JAK1 JH2, deucravacitinib elicited low functional activity in a JAK1/JAK3-dependent IL-2 stimulated cellular assay. BMS-986202 displays >10,000-fold selectivity for TYK2 JH2 over a diverse panel of 273 kinases and pseudokinases that include JAK family members. Like deucravacitinib, its high binding affinity to JAK1 JH2 (IC50 = 7.8 nM) did not translate to functional activity in the cellular assay.
Pharmacokinetics
The crystalline free base form of deucravacitinib exhibited poor aqueous solubility (5.2 μg/mL), which was still acceptable for preclinical studies. It showed moderate half-lives of 4?5 h across species (mouse, dog, and monkey). Excellent exposures and high bioavailability (F > 85%) in mice, dogs, and monkeys were obtained from oral pharmacokinetic studies at a 10 mpk dose. Following oral administration of deucravacitinib, the major metabolite in human plasma was the cyclopropyl carboxamide hydrolytic cleavage product 4 (6-amino-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-methylpyridazine-3-carboxamide).
BMS-986165 Preparation Products And Raw materials
Raw materials
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BMS-986165 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Dr. Reddy's Laboratories Ltd | +91-4049002900 +91-4049002900 | Hyderabad, India | 165 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| Zhengzhou Anbu Chem Co.,Ltd | +86-0371-88006763; +8615988602810 | China | 3000 | 58 | Inquiry |
| Hangzhou ICH Biofarm Co., Ltd | +86-0571-28186870; +undefined8613073685410 | China | 990 | 58 | Inquiry |
| hebei hongtan Biotechnology Co., Ltd | +86-86-1913198-3935 +8617331935328 | China | 973 | 58 | Inquiry |
| BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 +86-18600796368 | China | 227 | 58 | Inquiry |
| Jinan Jianfeng Chemical Co., Ltd | +8615562555968 | China | 247 | 58 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | United States | 19892 | 58 | Inquiry |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 24099 | 58 | Inquiry |