For research use only. Not for therapeutic Use.
Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis[1][2][3].
Safimaltib (JNJ-67856633) is effective and highly bioavailable in both mouse and rat tumors, and in some cases led to tumor stasis.
Safimaltib 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[1][3].
Dose dependent inhibition of the generation of Tregs (CD4+CD25+FoxP3+) following CD3/28 stimulation was observed upon treatment with JNJ-67856633 suggesting a potential immune modulatory role of MALT1 inhibition[3].
| Catalog Number | I044413 |
| CAS Number | 2230273-76-2 |
| Synonyms | 1-(1-oxo-2H-isoquinolin-5-yl)-5-(trifluoromethyl)-N-[2-(trifluoromethyl)pyridin-4-yl]pyrazole-4-carboxamide |
| Molecular Formula | C20H11F6N5O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H11F6N5O2/c21-19(22,23)15-8-10(4-6-27-15)30-18(33)13-9-29-31(16(13)20(24,25)26)14-3-1-2-12-11(14)5-7-28-17(12)32/h1-9H,(H,28,32)(H,27,30,33) |
| InChIKey | APWRZPQBPCAXFP-UHFFFAOYSA-N |
| SMILES | C1=CC2=C(C=CNC2=O)C(=C1)N3C(=C(C=N3)C(=O)NC4=CC(=NC=C4)C(F)(F)F)C(F)(F)F |
| Reference | [1]. Virtual meeting delivers first time drug structures [2]. A Phase 1, First-in-Human, Open-Label Study of the Safety, Pharmacokinetics, and Pharmacodynamics of JNJ-67856633, an Inhibitor of MALT1, in Participants with NHL and CLL [3]. Abstract 5690: Discovery of JNJ-67856633: A novel, first-in-class MALT1 protease inhibitor for the treatment of B cell lymphomas |
