BET bromodomain inhibitor 1

目录号: HY-131061 纯度: 99.91%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。

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BET bromodomain inhibitor 1 Chemical Structure

CAS No. : 2411226-02-1

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Free Sample (0.1 - 0.2 mg)		Apply now
10 mM * 1 mL in DMSO	￥4180	In-stock
1 mg	￥1727	In-stock
5 mg	￥3800	In-stock
10 mg	￥6000	In-stock
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生物活性
纯度 & 产品资料
参考文献

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^[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)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Kasumi 1	IC₅₀	7.4 nM Compound: 38	Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
MM1.S	IC₅₀	15.9 nM Compound: 38	Antiproliferative activity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
MV4-11	IC₅₀	2.4 nM Compound: 38	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
RS4-11	IC₅₀	22.1 nM Compound: 38	Antiproliferative activity against human RS4:11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human RS4:11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]

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].

MCE 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 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^[1].
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^[1].
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^[1].

MCE 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 T_1/2 of 1.3 hours, a CL of 21.5 mL/min•kg, and a V_ss of 1464 mL/kg.

分子量

459.47

Formula

C₂₂H₁₉F₂N₃O₄S

CAS 号

2411226-02-1

性状

固体

颜色

White to off-white

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

细胞实验：

DMSO 中的溶解度 : 62.5 mg/mL (136.03 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.44 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。
方案二

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); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案三

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); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（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。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.91%

选择批次：

Data Sheet (633 KB) SDS (251 KB)

COA (203 KB) HNMR (173 KB) RP-HPLC (228 KB) LCMS (107 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

BET bromodomain inhibitor 1 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1764 mL	10.8821 mL	21.7642 mL	54.4105 mL
	5 mM	0.4353 mL	2.1764 mL	4.3528 mL	10.8821 mL
	10 mM	0.2176 mL	1.0882 mL	2.1764 mL	5.4411 mL
	15 mM	0.1451 mL	0.7255 mL	1.4509 mL	3.6274 mL
	20 mM	0.1088 mL	0.5441 mL	1.0882 mL	2.7205 mL
	25 mM	0.0871 mL	0.4353 mL	0.8706 mL	2.1764 mL
	30 mM	0.0725 mL	0.3627 mL	0.7255 mL	1.8137 mL
	40 mM	0.0544 mL	0.2721 mL	0.5441 mL	1.3603 mL
	50 mM	0.0435 mL	0.2176 mL	0.4353 mL	1.0882 mL
	60 mM	0.0363 mL	0.1814 mL	0.3627 mL	0.9068 mL
	80 mM	0.0272 mL	0.1360 mL	0.2721 mL	0.6801 mL
	100 mM	0.0218 mL	0.1088 mL	0.2176 mL	0.5441 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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上海工商

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

BET bromodomain inhibitor 1

Customer Review