TNG348 is a novel, oral, potent and selective ubiquitin-specific protease 1 (USP1) inhibitor for studies related to BRCA1/2 mutations and other homologous recombination defect (HRD)+ cancers. TNG348 induces cell death through a pathway that is distinct from PARPi and TNG348 demonstrates robust synergy when combined with first- or second-generation PARPi. Moreover, TNG348 exhibits strong tumor growth inhibition in combination with PARPi in BRCA1/2mut and HRD+ xenograft models as well as models of acquired PARPi resistance. TNG348 is well tolerated, no body weight loss was observed in in vivo studies.
| CAS Number | 2839740-79-1 |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Deubiquitinase Products |
|---|
| FT-3171
FT-3171 is a small molecule ubiquitin-specific protease 1 (USP1) inhibitor targeting a novel DNA damage repair (DDR) pathway for studies related to solid tumors. |
| BAY-728
BAY-728 serves as a negative control for BAY-805, a potent and selective USP21 inhibitor. |
| BAY-805
BAY-805 is a selective inhibitor of the ubiquitin-specific protease USP21 with high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common off-target enzymes. |
| USP1-IN-6
USP1-IN-6 is a USP1 inhibitor (IC50<50 nM). |
| USP1-IN-5
USP1-IN-5 is a USP1 inhibitor (IC50<50 nM). |
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