BETd-246|cas:2140289-17-2|西域试剂

BETd-246,98.04%

产品编号：Bellancom-115568| CAS NO：2140289-17-2| 分子式：C₄₈H₅₅N₁₁O₁₀| 分子量：946.02

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货号	价格	库存与货期
Bellancom-115568	￥6500.00	杭州北京（现货）
Bellancom-115568	￥9500.00	杭州北京（现货）
Bellancom-115568	￥19500.00	杭州北京（现货）
Bellancom-115568	￥29500.00	杭州北京（现货）

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BETd-246

产品介绍

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。

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.

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

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
(In Vivo)

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.

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

Animal Model:	“Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESR^E380Q, PR- and HER2-)).
Dosage:	5, 10 mg/kg
Administration:	IV, 3 times per week for 3 weeks.
Result:	Effectively inhibited WHIM24 tumor growth.

体内研究

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

Animal Model:	“Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESR^E380Q, PR- and HER2-)).
Dosage:	5, 10 mg/kg
Administration:	IV, 3 times per week for 3 weeks.
Result:	Effectively inhibited WHIM24 tumor growth.

体内研究

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

Animal Model:	“Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESR^E380Q, PR- and HER2-)).
Dosage:	5, 10 mg/kg
Administration:	IV, 3 times per week for 3 weeks.
Result:	Effectively inhibited WHIM24 tumor growth.

性状

Solid

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。