2. PROTAC PI3K/Akt/mTOR
  3. PROTACs Akt
  4. 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

CAS No. : 3035638-40-2

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规格 价格 是否有货
1 mg ￥3800
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MS15 的其他形式现货产品:

Customer Review

Other Forms of MS15:

MS15 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

  • 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.

MS15 相关抗体:

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
CAS 号
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)

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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.

Keywords:

MS153035638-40-2MS 15MS-15PROTACsAktPKBProtein kinase BKRAS/BRAFcancerSW620 cellsColo205HT-29SKMEL 239PANC-1 cellsInhibitorinhibitorinhibit

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目录号：
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