MK-8033 (hydrochloride)
更新时间：2021-07-26 18:31:23
采购访问：20次
| 常用名 | MK-8033盐酸盐 | CAS号 | 1283000-43-0 |
|---|---|---|---|
| 价格 | $需询单/100g $需询单/1kg $需询单/100kg $需询单/1000kg | 纯度 | 98.0% |
| 备货期 | 需询单 | 库存 | 询单 |
| 产品详情（用途，包装等）
用途： MK8033 Hcl 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-Metin 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. 物理化学性质： CAS号：1283000-43-0 常用中文名：MK-8033盐酸盐 常用英文名：MK-8033 (hydrochloride) 分子式：C25H22ClN5O3S 分子量：507.99200 密度：N/A 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：2-8℃ |
达阳化工（杭州）有限公司
认证状态：已认证供应商
商品数：50181件
电话：+86571-88938639
地址：浙江省杭州市西湖区文三路259号2栋9楼
地区： 浙江省 杭州市 西湖区
联系人：王小姐
联系人电话：+86-571-8893-8639
邮件：enquiry@dycnchem.com
网址：http://www.dycnchem.com
主要市场：Mainly in Southeast Asia and European and American markets
年贸易额：10 to 20 million USD
外贸占销售比例：90%
主要合作伙伴：
- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：MK-8033 hydrochloride
- 价格： ￥13800.9/50mg ￥5800.9/10mg ￥2386.9/2mg ￥3580.9/5mg
- 纯度：99.0%
- 备货期：10天
- 联系人：阿拉丁
- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：MK-8033(hydrochloride)
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
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参考价格：$510/10mM*1mLinDMSO