Cas No.: | 2230273-76-2 |
Chemical Name: | JNJ-67856633 |
Synonyms: | JNJ-6633 |
SMILES: | O=C(C1=C(C(F)(F)F)N(C2=CC=CC3=C2C=CNC3=O)N=C1)NC4=CC(C(F)(F)F)=NC=C4 |
Formula: | C20H11F6N5O2 |
M.Wt: | 467.32 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. JNJ-67856633 in some cases lead to tumor stasis[1][2][3]. |
Target: | MALT1 protease[1][2][3] |
In Vivo: | 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]. |
In Vitro: | JNJ-67856633 is effective and highly bioavailable in both mouse and rat tumors, and in some cases led to tumor stasis. 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[1][3]. |
References: | [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 |