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E6201

产品编号 T61755 CAS 603987-35-5

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].

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E6201, CAS 603987-35-5

规格	价格/CNY	货期
25 mg	￥ 10,600	10-14周
50 mg	￥ 13,800	10-14周
100 mg	￥ 17,500	10-14周

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生物活性

化学信息

存储 & 溶解度

产品描述	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.

分子量	389.44
分子式	C21H27NO6
CAS No.	603987-35-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

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稀释计算器

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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