JB170 - KKL Med Inc.

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JB170

目录号 : KM11736 纯度 : 98%

Data Sheet 产品使用指南

JB170 是一种强效且高度特异性的 PROTAC 介导的 AURORA-A 降解剂 (DC₅₀=28 nM)，通过将 Alisertib 连接至 Cereblon配体 Thalidomide 而形成。JB170 优先结合 AURORA-A (EC₅₀=193 nM) 而不是 AURORA-B (EC₅₀=1.4µM)。JB170 介导的 S 期阻滞是由 AURORA-A 耗竭引起的。JB170 对 AURORA-A 激酶的非催化功能具有很好的抑制能力。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC₅₀=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC₅₀=193 nM) over AURORA-B (EC₅₀=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.

体外研究

JB170 (1 μM; 24-72 hours; MV4-11 cells) mediates Aurora-A depletion inhibiting cancer cell survival.
JB170 (0.01-10 μM; 6 hours; MV4-11 cells) reduces AURORA-A levels .
JB170 (0.5 μM; 12 hours; MV4-11 cells) delays/arrests S-phase progression.
JB170 (0.5 μM; 0-72 hours; MV4-11 cells) induces apoptosis is exclusively caused by targeting AURORA-A.
JB170 (0.1 µM; 0-9 hours; IMR5 cells) shows rapid AURORA-A depletion. JB170 (0~1 μM; 6 hours; MV4-11 cells) strongly attenuates in mutants with respect to AURORA-A. JB170 (0.1 μM; 18 hours; MV4-11 cells) does not activate AURORA-A. JB170 (0~1 µM; 24 hours; IMR5 cells) largely abrogates AURORA-A depletion. JB170 (1 μM; 4 days; IMR5 cells) mediates Aurora-A depletion inhibiting cancer cell survival. JB170 (IMR5 cells) reduces AURORA-A levels by lowering AURORA-A mRNA levels.

Cell Viability Assay

Cell Line:	MV4-11 cells
Concentration:	1 µM
Incubation Time:	24-72 hours
Result:	After 72 hours, the number of viable cells was 32% of control levels.

Western Blot Analysis

Cell Line:	MV4-11 cells
Concentration:	0.01~10 μM
Incubation Time:	6 hours
Result:	Substantial degradation was observed at 100 nM and 1 µM.

Apoptosis Analysis

Cell Line:	MV4-11 cells
Concentration:	0.5 µM
Incubation Time:	0~72 hours
Result:	Apoptosis was exclusively caused by targeting AURORA-A.

Cell Cycle Analysis

Cell Line:	MV4-11 cells
Concentration:	0.5 µM
Incubation Time:	12 hours
Result:	Delayed or arrested S-phase progression.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (103.80 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0380 mL	5.1902 mL	10.3803 mL
5 mM	0.2076 mL	1.0380 mL	2.0761 mL
10 mM	0.1038 mL	0.5190 mL	1.0380 mL

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.60 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.60 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： 98%

Data Sheet

产品使用指南

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Other Forms of Rapamycin:

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