MK-8033

产品详情：

更新时间： 2025-08-23 11:17:45

CAS号：1001917-37-8

常用名： 3-(1-甲基-1H-吡唑-4-基)-5-氧代-N-(2-吡啶甲基)-5H-苯并[4,5]环己烯并[1,2-b]吡啶-7-甲磺酰胺

价格：
￥2723.0/5mg ￥15739.0/25mg ￥需询单/1g ￥5399.0/10mg

纯度： 98.0%

备货期： 1天

库存： 现货

产品页： http://www.aladdin-e.com/zh_cn/M127968.html

其他详情（用途，包装）：
用途： MK8033 is a novel and specific dual ATP competitive c-Met/Ron inhibitor (IC50=1 nM Wt c-Met) under investigation as a treatment for cancer.IC50 Value: 1 nM (Wt c-Met); 2.0 nM (c-Met N1100Y) [1]Target: c-Met/Ronin vitro: MK-8033 binds 3-fold more tightly to phosphorylated c-Met kinase domain (Kd= 3.2 nM) than to its unphosphorylated counterpart (Kd = 10.4 nM). Signigicantly, MK-8033 potently inhibits kinase activity of three oncogenic c-Met activation loop mutants, Y1230C, Y1230H, and Y1235D (IC50s ranging from 0.6 to 1 nM at 50 uM ATP) in addition to other c-Met activating mutants N1100Y and M1250T. MK-8033 potently inhibited GTL-16 proliferation with an IC50 of 582 ± 30 nM. By contrast the HCT116 cell line, which does not harbor basal c-Met activation, was not inhibited by MK-8033 (IC50 > 10000 nM) [1]. MK-8033 radiosensitized the high-c-Met-expressing EBC-1 and H1993 cells but not the low-c-Met-expressing cell lines A549 and H460. However, irradiation of A549 and H460 cells increased the expression of c-Met protein at 30 minutes after the irradiation. Subsequent targeting of this up-regulated c-Met by using MK-8033 followed by a second radiation dose reduced the clonogenic survival of both A549 and H460 cells. MK-8033reduced the levels of radiation-induced phosphorylated (activated) c-Met in A549 cells [2].in vivo: MK-8033 was orally dosed in GTL-16 tumor xenograft bearing mice. Mice were euthanized 1 h after dosing and tested for p-Met (Y1349) in tumors and MK-8033 concentrations in plasma. At 100 mg/kg,essentially complete inhibition of p-Met (Y1349) was achieved. An in vivo IC50 of 1.3 uM was deduced from the relationship between plasma MK-8033 level and Met pY1349. Treatment with escalating dosed of MK-8033 for 21 days lead to antitumor efficacies in a dose-dependent manner. Dosing at 3, 10, 30, and 100 mg/kg resulted in 22, 18, 57, and 86% tumor growth inhibition, respectively, relative to tumor from vehicle-treated mice.signatures. 物理化学性质： CAS号：1001917-37-8 常用中文名：3-(1-甲基-1H-吡唑-4-基)-5-氧代-N-(2-吡啶甲基)-5H-苯并[4,5]环己烯并[1,2-b]吡啶-7-甲磺酰胺常用英文名：MK-8033 分子式：C25H21N5O3S 分子量：471.53100 密度：1.39 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：2-8℃

供应商信息：

公司名：上海阿拉丁生化科技股份有限公司推荐

认证状态： 已认证供应商

商品数： 165907件

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地区： 上海市浦东新区

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公司介绍：
阿拉丁（A股科创板上市企业，股票代码：688179）是科研服务领域的领先供应商与制造商，拥有科学服务领域领导品牌：阿拉丁。核心业务涵盖高端化学与生化试剂、生命科学、小分子及化合物库及材料科学四大领域，并自主拥有“芯硅谷”实验耗材品牌，依托电商平台实现线上主导的销售模式。产品广泛服务于985/211高校、科研院所及生物医药、化工材料等领域220余家A股上市公司。
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其他供应商价格：

2024-07-15 价格：需询单 MK-8033

2021-02-06 价格：￥16549.0 MK-8033

2023-09-27 价格：￥需询单 MK8033

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3-(1-甲基-1H-吡唑-4-基)-5-氧代-N-(2-吡啶甲基)-5H-苯并[4,5]环己烯并[1,2-b]吡啶-7-甲磺酰胺价格

MK-8033

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