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首页-小分子抑制剂&激动剂-NF-κB Pathway-MALT1-SGR-1505
SGR-1505

Chemical Structure : SGR-1505

CAS No.: 2661481-41-8

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SGR-1505 (SGR1505)

货号: PC-25809Not For Human Use, Lab Use Only.

SGR-1505 (SGR1505) is a highly potent, allosteric MALT1 (paracaspase 1, PCASP1) inhibitor with biochemical IC50 of 1.3 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SGR-1505 (SGR1505) is a highly potent, allosteric MALT1 (paracaspase 1, PCASP1) inhibitor with biochemical IC50 of 1.3 nM.
SGR-1505 shows excellent selectivity against a panel of 17 human proteases (all IC50 values >10 μM).
SGR-1505 also demonstrats high selectivity against a kinase profiling panel of 468 human kinases and disease-relevant mutant variants.
SGR-1505 shows high cellular potency in BCL10 cleavage, IL-10 secretion, and cell viability assays using ABC-DLBCL cell lines OCI-LY3 and OCI-LY10 (IC50=10-120 nM).
SGR-1505 inhibits luciferase activity of the NF-κB reporter in Jurkat cells with IC5 of 36 nM.
SGR-1505 displays potent IL-2 inhibition with an IC50 of 18 nM in activated T-cell cytokine secretion assays in human peripheral blood mononuclear cells (PBMCs).
SGR-1505 at 75 mg/kg (three times daily, TID) suppressed tumor growth in a dose-dependent manner in OCI-LY3 xenograft model.

物理化学性质&存储条件

分子量 481.80
分子式 C18H12ClF4N9O
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

(R)-N-(5-Chloro-6-(2H-1,2,3-triazol-2-yl)pyridin-3-yl)-2-fluoro-8-methyl-8-(trifluoromethyl)-7,8-dihydro-6H-pyrazolo[1,5-a]pyrrolo[2,3-e]pyrimidine-6-carboxamide

参考文献

1. Nie Z, et al. J Med Chem. 2025 Nov 27;68(22):23977-23992.

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