BET bromodomain inhibitor 1

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BET bromodomain inhibitor 1  纯度: 99.91%

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 (Kd 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。

BET bromodomain inhibitor 1

BET bromodomain inhibitor 1 Chemical Structure

CAS No. : 2411226-02-1

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BET bromodomain inhibitor 1 相关产品

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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 (Kd 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[1].

IC50 & Target[1]

BRD4

2.6 nM (IC50)

BRD2(2)

1.3 nM (Kd)

BRD3(2)

1.0 nM (Kd)

BRD4(1)

3.0 nM (Kd)

BRD4(2)

1.6 nM (Kd)

BRDT(2)

2.1 nM (Kd)

体外研究
(In Vitro)

BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest[1].
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[1].
BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6[1].
BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC50>20 μM)[1].
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)[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

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[1]

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[1]

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[1].
BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T1/2 of 1.3 and 0.9 hours, a CL of 21.5 and 15.3 mL/min•kg, and a Vss of 1464 and 782 mL/kg for rats and mouse, respectively[1].
BET bromodomain inhibitor 1 (3 mg/kg; PO) has a T1/2 of 3.6 hours, a Cmax of 159 ng/mL and an AUC of 884 ng•h/mL for rats[1].
BET bromodomain inhibitor 1 (1.3 mg/kg; PO) has a T1/2 of 1.3 hours, a Cmax of 399 ng/mL and an AUC of 1710 ng•h/mL for mouse[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: An MV4-11 mouse xenograft model[1]
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[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T1/2 of 1.3 hours, a CL of 21.5 mL/min•kg, and a Vss of 1464 mL/kg.

分子量

459.47

Formula

C22H19F2N3O4S

CAS 号

2411226-02-1

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 : 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
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Zizhou Li, et al. Discovery of 8-Methyl-pyrrolo[1,2- a]pyrazin-1(2 H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors. J Med Chem. 2020 Apr 23;63(8):3956-3975.

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