BET bromodomain inhibitor 1|cas:2411226-02-1|西域试剂

BET bromodomain inhibitor 1,99.91%

产品编号：Bellancom-131061| CAS NO：2411226-02-1| 分子式：C₂₂H₁₉F₂N₃O₄S| 分子量：459.47

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货号	价格	库存与货期
Bellancom-131061	￥3800.00	杭州北京（现货）
Bellancom-131061	￥6000.00	杭州北京（现货）
Bellancom-131061	￥11500.00	杭州北京（现货）

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BET bromodomain inhibitor 1

产品介绍

BET bromodomain inhibitor 1 是一种具有口服活性的，选择性 BET 溴结构域抑制剂，对 BRD4 的 IC₅₀ 为 2.6 nM。BET bromodomain inhibitor 1 与 BRD2(2)，BRD3(2)，BRD4(1)，BRD4(2) 和 BRDT(2) 高亲和力结合 (K_d 值分别为 1.3 nM、1.0 nM、3.0 nM、1.6 nM、2.1 nM)。BET bromodomain inhibitor 1 具有抗癌活性。

生物活性

BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀ of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (K_d values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.

体外研究

BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest.
BET bromodomain inhibitor 1 (31.25-500 nM; 6 or 24 hours) is highly effective in inducing dose-dependent inhibition on c-Myc expression and upregulation of p21 levels.
BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6.
BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC₅₀>20 μM).
BET bromodomain inhibitor 1 demonstrates an excellent selectivity for the BET bromodomain family over other bromodomains, with an ∼1500-fold selectivity for BRD4(1) over EP300 (IC₅₀=3857 nM).
BET bromodomain inhibitor 1 strongly inhibited the growth of acute myeloid leukemia cell line MV4-11, acute leukemia cell lines Kasumi-1 and RS-4-11, and multiple myeloma cancer cell line MM1.S cells with IC₅₀ values of 2.4, 4.8, 17.6 and 15.1 nM, respectively.

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

Cell Cycle Analysis

Cell Line:	MV-4-11 cells
Concentration:	31.25, 62.5, 125 nM
Incubation Time:	24 hours
Result:	Led to more pronounced G1-phase cell cycle arrest.

Western Blot Analysis

Cell Line:	MV-4-11 cells
Concentration:	31.25, 62.5, 125, 250, 500 nM
Incubation Time:	6 or 24 hours
Result:	Induced dose-dependent inhibition on c-Myc expression and upregulation of p21 levels.

RT-PCR

Cell Line:	MV-4-11 cells
Concentration:	31.25, 62.5, 125 nM
Incubation Time:	6 hours
Result:	Robustly reduced the expressions of c-Myc, BCL-2, and CDK6.

体内研究
(In Vivo)

BET bromodomain inhibitor 1 (compound 38; 6.25, 12.5 mg/kg; PO; daily ; for 28 days) exhibits stronger antitumor activities and completely inhibits the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg.
BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T_1/2 of 1.3 and 0.9 hours, a CL of 21.5 and 15.3 mL/min•kg, and a V_ss of 1464 and 782 mL/kg for rats and mouse, respectively.
BET bromodomain inhibitor 1 (3 mg/kg; PO) has a T_1/2 of 3.6 hours, a C_max of 159 ng/mL and an AUC of 884 ng•h/mL for rats.
BET bromodomain inhibitor 1 (1.3 mg/kg; PO) has a T_1/2 of 1.3 hours, a C_max of 399 ng/mL and an AUC of 1710 ng•h/mL for mouse.

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

Animal Model:	An MV4-11 mouse xenograft model
Dosage:	6.25, 12.5 mg/kg
Administration:	PO; daily ; for 28 days
Result:	Exhibited stronger antitumor activities and completely inhibited the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg.

Animal Model:	Male SD rats
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	IV
Result:	Had a T_1/2 of 1.3 hours, a CL of 21.5 mL/min•kg, and a V_ss of 1464 mL/kg.

体内研究

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

Animal Model:	An MV4-11 mouse xenograft model
Dosage:	6.25, 12.5 mg/kg
Administration:	PO; daily ; for 28 days
Result:	Exhibited stronger antitumor activities and completely inhibited the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg.

Animal Model:	Male SD rats
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	IV
Result:	Had a T_1/2 of 1.3 hours, a CL of 21.5 mL/min•kg, and a V_ss of 1464 mL/kg.

体内研究

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

Animal Model:	An MV4-11 mouse xenograft model
Dosage:	6.25, 12.5 mg/kg
Administration:	PO; daily ; for 28 days
Result:	Exhibited stronger antitumor activities and completely inhibited the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg.

Animal Model:	Male SD rats
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	IV
Result:	Had a T_1/2 of 1.3 hours, a CL of 21.5 mL/min•kg, and a V_ss of 1464 mL/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (136.03 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1764 mL	10.8821 mL	21.7642 mL
5 mM	0.4353 mL	2.1764 mL	4.3528 mL
10 mM	0.2176 mL	1.0882 mL	2.1764 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 (5.44 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.44 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。
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.53 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.53 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明