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CAS No.: 1353552-97-2

Poseltinib Catalog No. CSN20296

Synonyms: HM71224;LY3337641

Poseltinib is a tyrosine kinase inhibitor of Bruton's tyrosine kinase (BTK).

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技术信息

生物活性

描述Bruton's tyrosine kinase (BTK), a member of the Tec family of tyrosine kinases and expressed in B cells, macrophages, and monocytes but not in T cells, plays a crucial role in signaling through the B cell receptor (BCR) and the Fcγ receptor (FcγR) in B cells and myeloid cells, respectively^[3]. Poseltinib, an orally active, selective and irreversible BTK inhibitor with an IC₅₀ value of 1.95 nM^[4]. Poseltinib effectively suppressed splenic B220⁺GL7⁺, B220⁺CD138⁺, and B220⁺CD69⁺B cell counts, and anti-dsDNA IgG and reduced splenomegaly and lymph node enlargement. It also prevented skin lesions caused by lupus development, ameliorated renal inflammation and damage with increased blood urea nitrogen and creatinine, and decreased proteinuria. Furthermore, Poseltinib also decreased mortality from lupus development in both mouse models. Those results indicated that inhibition of BTK by Poseltinib effectively reduced B cell hyperactivity and significantly attenuated the development of SLE (Systemic lupus erythematosus) and LN (lupus nephritis) in rodent SLE models^[4].
作用机制Poseltinib may covalently bind to the active site (cysteine 481 residue) of BTK.
参考文献

[1] NCT03099148
[2] NCT02628028
[3] Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L. Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases. J Med Chem. 2019 Sep 12;62(17):7643-7655. doi: 10.1021/acs.jmedchem.9b00794. Epub 2019 Aug 15. PMID: 31368705.
[4] Kim YY, Park KT, Jang SY, Lee KH, Byun JY, Suh KH, Lee YM, Kim YH, Hwang KW. HM71224, a selective Bruton's tyrosine kinase inhibitor, attenuates the development of murine lupus. Arthritis Res Ther. 2017 Sep 26;19(1):211. doi: 10.1186/s13075-017-1402-1. PMID: 28950886; PMCID: PMC5615432.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1253 mL
- 10.6265 mL
- 21.2529 mL
- 5 mM
- 0.4251 mL
- 2.1253 mL
- 4.2506 mL
- 10 mM
- 0.2125 mL
- 1.0626 mL
- 2.1253 mL

技术信息

CAS号

1353552-97-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H26N6O3

运输

蓝冰

分子量

470.52

别名

HM71224;LY3337641

溶解度

DMSO	77.5 mg/mL (164.7 mM)
Water	insoluble

动物实验配方

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