MS170|cas:2376136-61-5|西域试剂

MS170

产品编号：Bellancom-145282| CAS NO：2376136-61-5| 分子式：C₄₅H₅₆ClN₉O₇| 分子量：870.44

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-145282		￥5800.00	杭州北京（现货）
Bellancom-145282		￥10500.00	杭州北京（现货）

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MS170

产品介绍

MS170 是一种有效的选择性 PROTAC AKT 降解剂。MS170 消耗细胞总 AKT (T-AKT)，DC₅₀ 值为 32 nM。MS170 与 AKT1、AKT2 和 AKT3 结合，K_d 分别为 1.3 nM、77 nM 和 6.5 nM。

生物活性

MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC₅₀ value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with K_ds of 1.3 nM, 77 nM, and 6.5 nM, respectively.

体外研究

Cereblon (CRBN)-recruiting degrader MS170 is an effective AKT degrader without a ″hook effect″. MS170 selectively induces robust AKT protein degradation, inhibits downstream signaling, and suppresses cancer cell proliferation. MS170 concentration- and time-dependently induces AKT degradation through the ubiquitin-proteasome system (UPS).
MS170 (10 nM-10 μM) effectively inhibits the proliferation in multiple cancer cell lines.
MS170 (1 nM-10 μM) concentration-dependently depletes cellular total AKT (T-AKT) with the DC₅₀ value of 32±18 nM.

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

Cell Proliferation Assay

Cell Line:	BT474, PC3, and MDA-MB-468 cells
Concentration:	10 nM, 100 nM, 1 μM, 10 μM
Incubation Time:	5 days
Result:	Inhibited the cell growth with GI₅₀s of 0.7±0.2 μM, 7.4±2.2 μM, and 5.7±2.4 μM for BT474 cells, PC3 cells, and MDA-MB-468 cells, respectively.

Western Blot Analysis

Cell Line:	BT474 cells
Concentration:	1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM , 3 μM, and 10 μM
Incubation Time:	24 hours
Result:	Potently induced AKT degradation.

体内研究
(In Vivo)

MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection.

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

Animal Model:	Male Swiss albino mice
Dosage:	Single 50 mg/kg(Pharmacokinetic Analysis)
Administration:	IP injection over 8 h
Result:	Bioavailable in mouse PK studies. The C_max is1.4 μM at 2 h.

体内研究

MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection.

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

Animal Model:	Male Swiss albino mice
Dosage:	Single 50 mg/kg(Pharmacokinetic Analysis)
Administration:	IP injection over 8 h
Result:	Bioavailable in mouse PK studies. The C_max is1.4 μM at 2 h.

体内研究

MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection.

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

Animal Model:	Male Swiss albino mice
Dosage:	Single 50 mg/kg(Pharmacokinetic Analysis)
Administration:	IP injection over 8 h
Result:	Bioavailable in mouse PK studies. The C_max is1.4 μM at 2 h.