1. PROTAC PI3K/Akt/mTOR
  2. PROTACs Akt
  3. MS21

MS21 是一种有效的 AKT PROTAC 降解剂。MS21 可抑制 PI3K/PTEN 通路突变,以及抑制肿瘤细胞增殖,诱导细胞周期阻滞。MS21 具有抗肿瘤活性。(Pink: AKT ligand-2 (HY-48682); Black: Linker (HY-W014125); Blue: (S,R,S)-AHPC (HY-125845))

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MS21 Chemical Structure

MS21 Chemical Structure

CAS No. : 2376137-05-0

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1 mg ¥2650
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查看 PROTACs 亚型特异性产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MS21 is an effective AKT PROTAC degrader. MS21 can inhibit mutations in the PI3K/PTEN pathway, suppress the proliferation and induce cell cycle arrest of tumor cells. MS21 has anti-tumor activity. (Pink: AKT ligand-2 (HY-48682); Black: Linker (HY-W014125); Blue: (S,R,S)-AHPC (HY-125845))[1].

体外研究
(In Vitro)

MS21 (1-1000 nM; 24 小时) 在 PC-3 (DC50: 8.8 nM) 和 BT474 细胞中抑制 AKT 蛋白水平,以及下游信号传导[1]
MS21 (0.1-10 μM; 2-17 天) 可抑制 PC-3、MDA-MB-468 等多种细胞系的增殖,诱导细胞周期阻滞[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 1, 3, 10, 30, 100, 300 and 1000 nM
Incubation Time: 24 h
Result: Inhibited the level of T-Akt in a concentration‐dependent manner.
体内研究
(In Vivo)

MS21 (75 mg/kg; 腹腔注射; 21 天) 在 PC-3/MDA-MB-468 异种移植瘤裸鼠模型中具有抗肿瘤的活性,可降低肿瘤组织中 T-AKT 蛋白水平,且耐受性良好[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PC-3/MDA-MB-468 treated Nude mice[1]
Dosage: 75 mg/kg
Administration: Intraperitoneal injection (i.p.); 21 days
Result: Led to more than 90% tumor growth inhibition relative to vehicle treatment in PC-3 xenograft model and more than 80% in MDA-MB-468 xenograft model.
Reduced T-AKT protein levels in tumors, inhibited downstream signaling such as p-S6, decreased Ki67 staining, and somewhat upregulated the apoptosis marker cleaved caspase-3.
Did not cause significant weight loss or other overt toxicities, and the increase in blood glucose levels after treatment was less than that of AZD5363 (HY-15431).
分子量

1107.84

Formula

C58H79ClN12O6S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

Methanol 中的溶解度 : 95 mg/mL (85.75 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9027 mL 4.5133 mL 9.0266 mL
5 mM 0.1805 mL 0.9027 mL 1.8053 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.88%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Methanol 1 mM 0.9027 mL 4.5133 mL 9.0266 mL 22.5664 mL
5 mM 0.1805 mL 0.9027 mL 1.8053 mL 4.5133 mL
10 mM 0.0903 mL 0.4513 mL 0.9027 mL 2.2566 mL
15 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5044 mL
20 mM 0.0451 mL 0.2257 mL 0.4513 mL 1.1283 mL
25 mM 0.0361 mL 0.1805 mL 0.3611 mL 0.9027 mL
30 mM 0.0301 mL 0.1504 mL 0.3009 mL 0.7522 mL
40 mM 0.0226 mL 0.1128 mL 0.2257 mL 0.5642 mL
50 mM 0.0181 mL 0.0903 mL 0.1805 mL 0.4513 mL
60 mM 0.0150 mL 0.0752 mL 0.1504 mL 0.3761 mL
80 mM 0.0113 mL 0.0564 mL 0.1128 mL 0.2821 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MS21
目录号:
HY-141807
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