ZT-12-037-01

产品编号: DC26117 Featured
ZT-12-037-01
结构式
2328073-61-4
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中国地区超过5000个高品质化合物库存
应用领域
ZT-12-037-01 是靶向选择性丝氨酸/苏氨酸激酶 STK19 抑制剂,与 STK19 蛋白具有高亲和力相互作用,抑制 NRAS 驱动的黑素细胞恶性转化。ZT-12-037-01 是ATP 竞争性抑制剂,可以抑制 NRAS 的磷酸化,IC50 为24 nM。
Cas No.: 2328073-61-4
名称: N2-cyclopropyl-N4-(1-isopropylpiperidin-4-yl)-6,7-dimethoxyquinazoline-2,4-diamine
别名:
SMILES: COC1=CC2=NC(NC3CC3)=NC(NC4CCN(C(C)C)CC4)=C2C=C1OC
分子式: C21H31N5O2
分子量: 385.512
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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