| Identification | Back Directory | [Name]
ZT-12-037-01 | [CAS]
2328073-61-4 | [Synonyms]
ZT-12-037-01
2,4-Quinazolinediamine, N2-cyclopropyl-6,7-dimethoxy-N4-[1-(1-methylethyl)-4-piperidinyl]- | [Molecular Formula]
C21H31N5O2 | [MDL Number]
MFCD32197197 | [MOL File]
2328073-61-4.mol | [Molecular Weight]
385.5 |
| Chemical Properties | Back Directory | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
DMSO: 8.33 mg/mL (21.61 mM) | [form ]
Solid | [color ]
White to off-white | [InChI]
1S/C21H31N5O2/c1-13(2)26-9-7-15(8-10-26)22-20-16-11-18(27-3)19(28-4)12-17(16)24-21(25-20)23-14-5-6-14/h11-15H,5-10H2,1-4H3,(H2,22,23,24,25) | [InChIKey]
AMAQJTHMSLYMFT-UHFFFAOYSA-N | [SMILES]
N1(CCC(CC1)Nc2nc(nc4c2cc(c(c4)OC)OC)NC3CC3)C(C)C |
| Hazard Information | Back Directory | [Uses]
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM[1]. | [Biological Activity]
ZT-12-037-01 is an ATP-competitive STK19 inhibitor with IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. At a concentration of 1 μM, it is highly selective against a kinase library of 468 kinases. | [in vitro]
Treatment with ZT-12-037-01 could effectively inhibit NRAS phosphorylation. ZT-12-037-01 is an ATP-competitive inhibitor that potently inhibits melanocytic colony formation, proliferation and tumor formation driven by mutant NRAS-STK19. It's pro-apoptotic activity was significantly enhanced in cells expressing oncogenic NRAS. | [in vivo]
ZT-12-037-01 is a potent STK19 inhibitor with low toxicity in vivo. In the SK-MEL-2 xenograft model (carrying NRAS. | [target]
| Target | Value | STK19
(Cell-free assay) | 23.96 nM | STK19 (D89N)
(Cell-free assay) | 27.94 nM | < /table>[References]
[1] Yin C, et al. Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell. 2019 Feb 21;176(5):1113-1127.e16. DOI:10.1016/j.cell.2019.01.002 |
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Tags:2328073-61-4
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