1. PROTAC PI3K/Akt/mTOR
  2. PROTACs Akt
  3. MS15

MS15 是一种有效且选择性的 AKT PROTAC 降解剂。 MS15 可抑制 AKT1、-2 和 -3 活性,IC50 值分别为 798 nM、90 nM 和 544 nM。

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MS15 Chemical Structure

MS15 Chemical Structure

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1 mg ¥3800
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5 mg ¥9300
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively[1].

IC50 & Target

Akt2

90 ± 2.8 nM (IC50)

Akt3

544 ± 2.9 nM (IC50)

Akt1

798 ± 190 nM (IC50)

体外研究
(In Vitro)

MS15 (0-10 μM, 24 h) potently induces AKT degradation in SW620 cells and MS21-resistant KRAS/BRAF mutant cells[1].
MS15 (0-10 μM, 5 days) inhibits the proliferation of KRAS mutant SW620 cells[1].
MS15 (1 μM, 1-24 h) mediates AKT degradation in a time- and UPS-dependent manner[1].

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

Western Blot Analysis[1]

Cell Line: SW620 cells, Colo205, HT-29, SKMEL 239, and PANC-1 cells
Concentration: 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM
Incubation Time: 24 h
Result: Effectively induced T-AKT degradation in a concentration-dependent manner, with a DC50 value of 23 ± 16 nM in SW620 cells. Nearly complete AKT degradation was achieved at a concentration of 100 nM in SW620 cells and PANC-1 cells. Induced AKT degradation at 1 μM in BRAF mutant cell lines, such as Colo205, HT-29, and SKMEL 239 cells.

Cell Proliferation Assay[1]

Cell Line: SW620 cells
Concentration: 0 nM, 30 nM, 100 nM, 1 μM, 3 μM, 10 μM
Incubation Time: 5 days
Result: Displayed slightly better antiproliferative activity than Miransertib (HY-19719), with a GI50 of 3.1 ± 0.3 μM.
体内研究
(In Vivo)

MS15 (75 mg/kg, IP, once) is bioavailable in mice through intraperitoneal administration[1].

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

Animal Model: Male Swiss albino mice[1]
Dosage: 75 mg/kg
Administration: IP, once (Pharmacokinetic Analysis)
Result: The maximum plasma concentration (Cmax = 1 μM) was achieved at 0.5 h post-treatment, and plasma concentrations were maintained above 100 nM for at least 12 h.Could achieve enough plasma exposure for effective AKT degradation.
分子量

1114.45

Formula

C64H79N11O5S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

MS15 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:
MS15
目录号:
HY-151613
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