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  • 化合物 E6201|T61755|TargetMol

化合物 E6201|T61755|TargetMol

E6201
603987-35-5
￥10600 25mg 起订
￥13800 50mg 起订
￥17500 100mg 起订
上海 更新日期：2024-09-30

TargetMol中国（陶术生物）

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联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 E6201
英文名称：
E6201
CAS号：
603987-35-5
品牌：
TargetMol
产地：
美国
保存条件：
Shipping with blue ice.
产品类别：
抑制剂
货号：
T61755

Product Introduction

Bioactivity

名称E6201
描述E6201 (ER-806201) is a potent dual kinase inhibitor targeting MEK1 and FLT3, inhibiting their activities in an ATP-competitive manner. It effectively suppresses MEK1-induced ERK2 phosphorylation (IC50 = 5.2 nM), MKK4-induced JNK phosphorylation (IC50 = 91 nM), and MKK6-induced p38 MAPK phosphorylation (IC50 = 19 nM). E6201 exhibits anti-tumor and anti-psoriasis effects [1] [2].
体外活性E6201 is an inhibitor of MEKK1 and MEK families but not the MAPK family. E6201 inhibits MEKK1- induced phosphorylation of MEK1, MKK4, and MKK6 with IC 50 values of 31, 522, and 65 nM, respectively. E6201 has no effect on other MAPK family enzymes such as ERK2, JNKs, and p38 MAPK at 10 μM [1]. E6201 inhibits LPS-induced TNF transcription with an IC 50 value of 50±14 nM, but does not suppress β-actin transcription at 3 μM and only slightly at 10 μM [1]. E6201 inhibits the receptor tyrosine kinases VEGFR2, PDGFR, hepatocyte growth factor receptor, and EGFR with IC 50 values of 350, 860, 1100, and 5400 nM, respectively, as well as the nonreceptor tyrosine kinase Syk with an IC 50 value of 460 nM. E6201 does not inhibit ZAP-70 or IKK at 10 μM or PKC activity at 100 μM [1]. E6201 inhibits IL-2 production 48 h after stimulation with the T-cell mitogen PHA-P, with an IC 50 value of 18 nM [1]. E6201 inhibits the proliferation of EGF-stimulated human keratinocytes with an IC 50 value of 160 nM [1]. E6201 suppresses IL-8 production in human keratinocytes 24 h after stimulation with IL-1α or TNFα, with IC 50 values of 60 and 30 nM, respectively [1]. E6201 inhibits TNFα, IL-1, IL-6, and IL-8 production from human PBMCs with IC 50 values of 20, 16, 52, and 53 nM, respectively [1]. E6201 (0.08-20.0 μM) significantly inhibited triple-negative breast cancer (TNBC) cell proliferation and anchorage-independent colony formation in a dose-dependent manner [2]. E6201 (1 μM) inhibits expression of phospho-ERK and induces G1 phase cell cycle arrest, and apoptosis in TNBC [2]. Cell Viability Assay [2] Cell Line: Human TNBC cell lines BT20, HCC70, MDA-MB-231, HCC1806, HCC1937, SUM149 and SUM159 Concentration: 0.00, 0.08, 0.16, 0.31, 0.63, 1.25, 2.50, 5.00, 10.0, 20.0 μM Incubation Time: 5 days Result: Inhibited TNBC cell proliferation and anchorage-independent colony formation in a dose-dependent manner. Western Blot Analysis [3] Cell Line: Human TNBC cell lines BT20, HCC70, MDA-MB-231, HCC1806, HCC1937, SUM149 and SUM159 Concentration: 1 μM Incubation Time: 0, 1, 24 hours Result: pERK expression level showed a rapid (apparent by 1 hour) and sustained (still apparent at 24 hours) decrease in the tested TNBC cell lines following treatment.
体内活性E6201 (30 mg/kg; administered via tail vein injection three times per week) inhibits TNBC xenograft tumor growth. E6201 strongly inhibits pERK and Ki-67 expression in xenograft tumor tissues [2]. Animal Model: Female Nod.Scid gamma mice (age 4 to 6 weeks old) bearing MDA-MB-231-LM2 xenograft tumors [2] Dosage: 30 mg/kg Administration: Administered via tail vein injection three times per week for 17 days Result: Compared with mice treated with vehicle control, the E6201-treated mice showed 60% tumor growth suppression.
存储条件Shipping with blue ice.
E6201|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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