ABBV-MALT1 | MALT1 inhibitor | Probechem Biochemicals

Chemical Structure : ABBV-MALT1

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ABBV-MALT1 (MALT1 inhibitor)

货号: PC-22030Not For Human Use, Lab Use Only.

ABBV-MALT1 is a potent, selective, allosteric inhibitor of the MALT1 paracaspase with binding KD of 37 nM, exhibits potent biochemical inhibition of MALT1 protease activity with IC50 of 349 nM.

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生物&药学活性

ABBV-MALT1 is a potent, selective, allosteric inhibitor of the MALT1 paracaspase with binding KD of 37 nM, exhibits potent biochemical inhibition of MALT1 protease activity with IC50 of 349 nM.
Displays no meaningful off-target activity against a panel of 177 kinases representing each branch of the kinome, 55 pharmacological receptor binding assays and four caspase activity assays.
ABBV-MALT1 effectively inhibits immune cell activation as measured by secreted IL-2 with EC50 of 300 nM in human PBMCs.
ABBV-MALT1 treatment completely inhibits the ability of T cells to express IFNy after co-stimulation with 10 ug/mL anti-PD1, with no effect on T cell viability.
ABBV-MALT1 selectively inhibitsthe growth of ABC subtype diffuse large B cell lymphoma (ABC-DLBCL) models (OCI-LY3 tumor cell line, EC50=300 nM) to varying maxima and shows no activity in GCBDLBCL cells, upregulates MALT1 substrates BCL10, RELB and ZC3H12D protein levelsin a dose-dependent manner in OCI-LY3 cells.
ABBV-MALT1 (30 mg/kg, twice daily for 14 days, oral) is efficacious in the OCILY10 CDX model (TGI of 73%), which harbors an activating CD79A mutation, combination of MALT1 and BCL2 inhibition is highly efficacious in vivo.

物理化学性质&存储条件

分子量	478.45
分子式	C19H17F3N8O2S
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	(S)-1-(6-(2H-1,2,3-triazol-2-yl)-5-(trifluoromethyl)pyridin-3-yl)-3-(7-(1-methoxyethyl)-2-methylthiazolo[5,4-b]pyridin-6-yl)urea

参考文献

1. Joshua P Plotnik, et al. Mol Cancer Ther. 2024 Mar 20. doi: 10.1158/1535-7163.MCT-23-0518.