ZT-12-037-01
ZT-12-037-01 Basic information
- Product Name:
- ZT-12-037-01
- Synonyms:
-
- ZT-12-037-01
- 2,4-Quinazolinediamine, N2-cyclopropyl-6,7-dimethoxy-N4-[1-(1-methylethyl)-4-piperidinyl]-
- inhibit,ZT 12 037 01,ZT1203701,Ras,Inhibitor
- N2-Cyclopropyl-N4-(1-isopropylpiperidin-4-yl)-6,7-dimethoxyquinazoline-2,4-diamine
- CAS:
- 2328073-61-4
- MF:
- C21H31N5O2
- MW:
- 385.5
- Mol File:
- 2328073-61-4.mol
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ZT-12-037-01 Chemical Properties
- storage temp.
- 2-8°C(protect from light)
- solubility
- DMSO: 8.33 mg/mL (21.61 mM)
- form
- Solid
- color
- White to off-white
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ZT-12-037-01 Usage And Synthesis
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.