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ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. ZT-12-037-01 effectively blocks oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vitro and in vivo. ZT-12-037-01 (3 μM; 14 days) significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation.
In vivo, ZT-12-037-01 (25-50 mg/kg; injection subcutaneously; once daily) 21 days treatment inhibits growth of SK-MEL-2 xenograft melanoma and the sections of tumors indicates induction of apoptosis by increasing cleaved caspase-3.
| Molecular Weight | 385.50 |
| Formula | C21H31N5O2 |
| CAS Number | 2328073-61-4 |
| Solubility (25°C) | DMSO ≥ 9 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Ras Products |
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| HRS-4642
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| HH0043
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Products are for research use only. Not for human use. We do not sell to patients.
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