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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-TUL01101
TUL01101

Chemical Structure : TUL01101

CAS No.: 2411222-97-2

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TUL01101 (Blovacitinib, TUL-01101)

货号: PC-25034Not For Human Use, Lab Use Only.

Blovacitinib (TUL01101) is a potent, selective and oral Janus kinase 1 (JAK1) inhibitor with IC50 of 3 nM, >12-fold selectivity for JAK2 and TYK2.

规格 价格 库存 数量
2 mg ￥2480 In stock
5 mg ￥3980 In stock
10 mg ￥5880 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Blovacitinib (TUL01101) is a potent, selective and oral Janus kinase 1 (JAK1) inhibitor with IC50 of 3 nM, >12-fold selectivity for JAK2 and TYK2.
TUL01101 interacts with JAK1 JH1 domain.
TUL01101 can effectively inhibit signaling pathways involved by JAK1 mediated by IL-6, with stronger inhibitory activity than filgotinib (IC50: 125.9 vs 407.4 nM).
TUL01101 can effectively inhibit JAK1-JAK3 signaling pathway mediated by IL-2 and JAK1-TYK2 signaling pathway mediated by IFNα.
TUL01101 does not inhibit JAK2 signaling pathways induced by GM-CSF.
TUL01101 (1 mg/kg, BID, p.o.) exhibited effective activity in the treatment of RA both in collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) models, with low dose and low toxicity.

物理化学性质&存储条件

分子量 429.47
分子式 C22H25F2N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-N-(5-(2-(2,2-difluorocyclopropane-1-carbonyl)-2-azaspiro[3.5]nonan-7-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide

参考文献

1. Shuhao Zhou, et al. J Med Chem. 2022 Dec 22;65(24):16716-16740.

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