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Safimaltib

Chemical Structure : Safimaltib

CAS No.: 2230273-76-2

Safimaltib (JNJ-67856633)

Catalog No.: 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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25 mg $218 In stock
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100 mg $558 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 467.331
Formula C20H11F6N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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