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ZT-12-037-01

  Cat. No.:  DC26117   Featured
Chemical Structure
2328073-61-4
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More than 5000 active chemicals with high quality for research!
Field of application
ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 of 20.04 nM measured as percentage of NRAS phosphorylation; shows similar IC50 of 23.96 and 27.94 nM for STK19WTWT STK19D89N respectively; displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 uM; efficiently inhibits phosphorylation of NRAS in a dose- and time-dependent manner, inhibits NRAS activity in a dose-dependent manner but does not affect the levels of H3K9 methylation; effectively inhibits NRAS signaling, including the MEK-ERK and PI3K pathways in SK-MEL-2 and WM2032 cells (with NRASQ61R), but the inhibition was much less effective in A375 or UACC62 cells (with NRASWT), effectively inhibits cell growth and induces apoptosis of SK-MEL-2 and WM2032 melanoma cells.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2328073-61-4
Chemical Name: N2-cyclopropyl-N4-(1-isopropylpiperidin-4-yl)-6,7-dimethoxyquinazoline-2,4-diamine
SMILES: COC1=CC2=NC(NC3CC3)=NC(NC4CCN(C(C)C)CC4)=C2C=C1OC
Formula: C21H31N5O2
M.Wt: 385.512
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Yin C, et al. Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell. 2019 Feb 21;176(5):1113-1127.e16.
Description: 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].
In Vivo: ZT-12-037-01 (injection subcutaneously; 25-50 mg/kg; once daily; 21 days) inhibits growth of SK-MEL-2 xenograft melanoma and the sections of tumors indicates induction of apoptosis by increasing cleaved caspase-3[1]. Animal Model: SK-MEL-2 xenograft melanoma nude mice with hTERT/p53DD/CDK4(R24C) melanocytes[1] Dosage: 25 mg/kg; 50 mg/kg Administration: Injected subcutaneously; 21 days Result: Inhibited growth of SK-MEL-2 xenograft melanoma.
In Vitro: ZT-12-037-01 (3 μM; 14 days) significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation[1]. ZT-12-037-01 (0-3 μM) has an inhibitory effects of ZT-12-037-01 on STK19WT and STK19D89N-activated NRAS phosphorylation in HPMs[1]. Cell Proliferation Assay[1] Cell Line: CDK4 (R24C) melanocyte cells; hTERT melanocyte cells; p53DD melanocyte cells Concentration: 3 μM Incubation Time: 14 days Result: Inhibited melanocyte proliferation. Western Blot Analysis[1] Cell Line: STK19WT and STK19D89N Concentration: 0 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM Incubation Time: Result: Inhibited NRAS phosphorylation.
References: [1]. Yin C, et al. Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell. 2019 Feb 21;176(5):1113-1127.e16.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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