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

Chemical Structure : Safimaltib

CAS No.: 2230273-76-2

Safimaltib (JNJ-67856633)

货号: PC-73444Not For Human Use, Lab Use Only.

Safimaltib (JNJ-67856633) is a potent, selective, allosteric inhibitor of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) protease activity.

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10 mg ¥1280 In stock
25 mg ¥2180 In stock
50 mg ¥3580 In stock
100 mg ¥5580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Safimaltib (JNJ-67856633) is a potent, selective, allosteric inhibitor of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) protease activity.
Safimaltib (JNJ-67856633) inhibits proliferation of activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL) cell lines bearing CD79b or CARD11 mutations as well as models mimicking resistance to covalent BTK inhibitors.
JNJ-67856633 showed activity in organoid cultures derived from ABC-DLBCL patients.
JNJ-67856633 leads to potent in vivo pharmacodynamic shutdown in CD79b- as well as CARD11-mutant ABC-DLBCL models as measured by serum IL10 or uncleaved BCL10 levels in tumors.
JNJ-67856633 exhibits potent tumor growth inhibition in two human DLBCL xenograft models, OCI Ly3 and OCI Ly10.

物理化学性质&存储条件

分子量 467.331
分子式 C20H11F6N5O2
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

1-(1-oxo-1,2-dihydroisoquinolin-5-yl)-5-(trifluoromethyl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1H-pyrazole-4-carboxamide

参考文献

1. Ulrike Philippar, et al. Cancer Res (2020) 80 (16_Supplement): 5690.

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