BETd-246 - CAS:2140289-17-2

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BETd-246

目录号 : KM7811 CAS No. : 2140289-17-2 纯度 : 98%

Data Sheet 产品使用指南

BETd-246 是第二代、基于 PROTAC 技术的、 BET溴端结构域 (BRD) 的抑制剂，由Cereblon配体和BET配体相连，具有良好的选择性、有效性和抗肿瘤活性。

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5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.

体外研究

BETd-246 treatment (0-100 nM, 1-3 h) causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation.
BETd-246 (100 nM, 24/48 hours) displays strong growth inhibition and apoptosis induction activity in MDA-MB-468 cell lines. BETd-246 induces a rapid and time-dependent downregulation of MCL1 protein in all the TNBC cell lines evaluated. BETd-246 induces much stronger apoptosis than BETi-211.
BETd-246 (100 nM, 24 hours) induces pronounced cell cycle arrest and apoptosis in TNBC cell lines.

Cell Proliferation Assay

Cell Line:	MDA-MB-468 cells
Concentration:	100 nM
Incubation Time:	24 or 48 hours
Result:	Displayed strong growth inhibition and apoptosis induction activity in TNBC cell lines.

Cell Cycle Analysis

Cell Line:	Human TNBC cells
Concentration:	100 nM
Incubation Time:	24 hours
Result:	Induced pronounced cell cycle arrest and apoptosis in TNBC cell lines.

Western Blot Analysis

Cell Line:	Human TNBC cells
Concentration:	0-100 nM
Incubation Time:	1-3 hours
Result:	Caused a dose-dependent depletion of BRD2, BRD3 and BRD4.

体内研究

BETd-246 (5 mg/kg, IV, 3 times per week for 3 weeks) treatment effectively inhibits WHIM24 tumor growth, similar to the antitumor activity of BETi-211 with higher dosage and more frequently administration. The treatment of 10 mg/kg induces partial tumor regression during treatment without apparent toxicity. BETd-246 has very limited drug exposure in the xenograft tumor tissue in MDA-M-231and MDA-MB-468 models.

Animal Model:	“Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESR, PR- and HER2-)).
Dosage:	5, 10 mg/kg
Administration:	IV, 3 times per week for 3 weeks.
Result:	Effectively inhibited WHIM24 tumor growth.

分子式

C₄₈H₅₅N₁₁O₁₀

分子量

946.02

CAS号

2140289-17-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : 200 mg/mL (211.41 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0571 mL	5.2853 mL	10.5706 mL
5 mM	0.2114 mL	1.0571 mL	2.1141 mL
10 mM	0.1057 mL	0.5285 mL	1.0571 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 (stored under nitrogen)。-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: ≥ 5 mg/mL (5.29 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (5.29 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。