JNJ-67856633 是口服有效的、选择性的、变构性的MALT1 Protease抑制剂。在某些情况下,JNJ-67856633可以导致肿瘤停滞。
产品描述
JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric inhibitor of MALT1 protease . JNJ-67856633 lead to tumor stasis in some cases.
体外活性
JNJ-67856633 is effective and highly bioavailable in both mouse and rat tumors, and in some cases led to tumor stasis. JNJ-67856633 results in 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].
体内活性
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].
Cas No.
2230273-76-2
分子式
C20H11F6N5O2
分子量
467.32
储存和溶解度
DMSO:125 mg/mL (267.48 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years