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MS1943 {[allProObj[0].p_purity_real_show]}

货号:A1327306 Ambeed 开学季,买赠积分,赢豪礼

MS1943 is a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells.

MS1943 化学结构 CAS号:2225938-17-8
MS1943 化学结构
CAS号:2225938-17-8
MS1943 3D分子结构
CAS号:2225938-17-8
MS1943 化学结构 CAS号:2225938-17-8
MS1943 3D分子结构 CAS号:2225938-17-8
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MS1943 纯度/质量文件 产品仅供科研

货号:A1327306 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

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Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

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Venlafaxine {[allProObj[0].p_purity_real_show]}
Fluvoxamine maleate {[allProObj[0].p_purity_real_show]}
Iloperidone {[allProObj[0].p_purity_real_show]}
Ziprasidone HCl {[allProObj[0].p_purity_real_show]}
Atomoxetine HCI +

5-HT, Ki: 77 nM

{[allProObj[0].p_purity_real_show]}
Dapoxetine HCl {[allProObj[0].p_purity_real_show]}
Trazodone {[allProObj[0].p_purity_real_show]}
Clomipramine HCl {[allProObj[0].p_purity_real_show]}
Mirtazapine {[allProObj[0].p_purity_real_show]}
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

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Duloxetine {[allProObj[0].p_purity_real_show]}
Sertraline HCl ++

5-HT, Ki: 13 nM

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Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

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Latrepirdine 2HCl GluR {[allProObj[0].p_purity_real_show]}
Fluoxetine HCl {[allProObj[0].p_purity_real_show]}
Paroxetine hydrochloride AChR {[allProObj[0].p_purity_real_show]}
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

+

5-HT2, pIC50: 5.5

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Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

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LY310762 +

5-HT1D, Ki: 249 nM

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Cyclobenzaprine HCI {[allProObj[0].p_purity_real_show]}
Blonanserin +++

5-HT2, Ki: 3.98 nM

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Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

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Olanzapine {[allProObj[0].p_purity_real_show]}
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

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Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

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Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

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Agomelatine {[allProObj[0].p_purity_real_show]}
Clozapine {[allProObj[0].p_purity_real_show]}
Amitriptyline +

5-HT2, Ki: 235 nM

SERT {[allProObj[0].p_purity_real_show]}
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

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RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

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Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

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Tropisetron {[allProObj[0].p_purity_real_show]}
Palonosetron {[allProObj[0].p_purity_real_show]}
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

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Ondansetron {[allProObj[0].p_purity_real_show]}
Granisetron {[allProObj[0].p_purity_real_show]}
Alosetron HCl {[allProObj[0].p_purity_real_show]}
Ondansetron hydrochloride dihydrate {[allProObj[0].p_purity_real_show]}
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

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Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

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Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

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Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

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SB 271046 HCl +++

5-HT6, pKi: 8.92

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Intepirdine ++++

5-HT6, pKi: 9.63

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SB-269970 HCl ++

5-HT7, pKi: 8.3

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BRL 15572 ++

5-HT1B, pKi: 6.1

5-HT1D, pKi: 6

++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Histone Methyltransferase 其他靶点 纯度
BRD4770 {[allProObj[0].p_purity_real_show]}
UNC1999 +++

EZH2, IC50: 2 nM

EZH1, IC50: 45 nM

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EPZ005687 ++

EZH2, Ki: 24 nM

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EPZ015666 +++

PRMT5, Ki: 5 nM

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3-Deazaneplanocin A HCl ++++

S-adenosylhomocysteine hydrolase, Ki: 50 pM

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EPZ6438 +++

EZH2, IC50: 11 nM

EZH2, Ki: 2.5 nM

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GSK126 ++

EZH2, IC50: 9.9 nM

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MI-3 +

Menin-MLL, IC50: 648 nM

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MM-102 ++

MLL1, IC50: 0.4 μM

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EI1 ++

Ezh2 (wild-type), IC50: 15 nM

EZH2 (Y641F), IC50: 13 nM

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SGC0946 ++++

DOT1L, IC50: 0.3 nM

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PFI-2 HCl ++++

SETD7, IC50: 2 nM

SETD7, Ki: 0.33 nM

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Pinometostat ++++

DOT1L, Ki: 80 pM

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EPZ004777 +++

DOT1L, IC50: 0.4 nM

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Entacapone ++

COMT, IC50: 151 nM

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UNC0379 +

SETD8, IC50: 7.9 μM

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Menin-MLL inhibitor MI-2 +

Menin-MLL, IC50: 446 nM

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GSK343 +++

EZH2, IC50: 4 nM

EZH1, IC50: 240 nM

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BIX-01294 3HCl +

G9a, IC50: 2.7 μM

{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

MS1943 生物活性

描述 MS1943 represents a pioneering orally bioavailable EZH2 selective degrader, demonstrating an IC50 value of 120 nM. It notably diminishes EZH2 protein levels across various triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. Additionally, MS1943 robustly impedes the proliferation of multiple TNBC and other cancer cell lines[1].
体内研究

MS1943 (150 mg/kg body weight; i.p.; once daily for 36 days) inhibits tumor growth[1].

MS1943 triggers apoptosis in the MDA-MB-468 xenograft model[1].

A sole intraperitoneal (i.p.) administration of MS1943 at 50 mg/kg body weight led to a peak plasma concentration (Cmax) of 2.9 µM, maintaining plasma concentrations above its cellular IC50 value for approximately 2 hours. Conversely, a single oral (p.o.) dose of 150 mg/kg body weight yielded a Cmax of 1.1 µM, with plasma concentrations falling below the cellular IC50 value[1].

体外研究

MS1943 (0.625-5 μM; 3 days) suppresses cell growth, yielding a GI50 value of 2.2 µM[1].

MS1943 (0.625-5 μM; 4 days) triggers cell death in MDA-MB-468 cells. Additionally, MS1943 efficiently decreases EZH2 levels in BT549, HCC70, and MDA-MB-231 TNBC cells, as well as in KARPAS-422 and SUDHL8 lymphoma cells, and PNT2 non-cancerous prostate cells[1].

MS1943 (1.25-5.0 μM; 2 days) decreases EZH2 and SUZ12 protein levels in a concentration- and time-dependent manner, while EED protein levels remain unaffected. Additionally, the H3K27me3 mark is suppressed[1].

MS1943 参考文献

[1]Ma A, et al. Discovery of a first-in-class EZH2 selective degrader.Nat Chem Biol. 2020 Feb;16(2):214-222.

MS1943 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.95mL

1.39mL

0.70mL

13.91mL

2.78mL

1.39mL

MS1943 技术信息

CAS号2225938-17-8
分子式C42H54N8O3
分子量 718.93
别名
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 120 mg/mL(166.91 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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