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BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research[1]. | [Definition]
BMS-502 is a dual DGKα and ζ inhibitor. BMS-502 demonstrated dose-dependent immune stimulation in the mouse OT-1 model, setting the stage for a drug discovery program. BMS-502 demonstrated substantial inhibitory activity against DGKs α, ζ and ι[1].
| [in vivo]
BMS-502 (Compound 22) (0-10mg/kg; PO; 24h) demonstrates dose-dependent immune stimulation in the mouse OT-1 model[1].
Pharmacokinetic Analysis in C57 black mice Model[1]
| Route | Dose (mg/kg) | AUClast (μM?h) | t1/2 (h) | Tmax (h) | Cmax (μM) | Cl (m/min/kg) | Vss (mL/kg) | F (%) | | i.v. | 1 | 14.8 | 22.5 | / | / | 1.9 | 3.9 | / | | p.o. | 5 | 48 | / | 3.0 | 1.08 | / | / | 65 |
| Animal Model: | OT-1 mouse model[1] | | Dosage: | 0-10 mg/kg | | Administration: | Oral administration; 24 h | | Result: | Caused no significant increase in activated effector T-cells. |
| [References]
[1] Louis Chupak* and Susan Wee. “Discovery of Potent, Dual-Inhibitors of Diacylglycerol Kinases Alpha and Zeta Guided by Phenotypic Optimization.” ACS Medicinal Chemistry Letters 14 7 (2023): 929–935.
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