1. PROTAC Epigenetics
  2. PROTACs Epigenetic Reader Domain
  3. BD-9136

BD-9136 是一种有效的和高选择性的 BRD4 PROTAC 降解剂。BD-9136 对 BRD4 具有低纳摩尔级的降解能力,对 BRD4 的降解选择性是 BRD2 和 BRD3 蛋白的 1000 倍。BD-9136 具有抗肿瘤的活性。(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))

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BD-9136 Chemical Structure

BD-9136 Chemical Structure

CAS No. : 3037514-38-5

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
1 mg ¥5350
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10 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BD-9136 is a potent and highly selective BRD4 PROTAC depressant. BD-9136 has low-nanomolar degradation potencies against BRD4 , and its degradation selectivity for BRD4 is 1000 times that of BRD2 and BRD3 proteins. BD-9136 has antitumor activity[1].(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))

体外研究
(In Vitro)

BD-9136 (0-1 μM;4 小时) 在 8 种肿瘤细胞系中可诱导 BRD4 降解,DC50 为 0.1-4.7 nM, Dmax > 90%,对 BRD2 和 BRD3 无降解作用[1]

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

Western Blot Analysis[1]

Cell Line: MV4;11 and MDAMB-231 cells
Concentration: 0, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 4 h
Result: Reduced the level of BRD4, but BRD2 and BRD3 did not change.
体内研究
(In Vivo)

BD-9136 (20 mg/kg;腹腔注射;一周 5 次共 4 周) 在肿瘤细胞异种移植小鼠模型中具有抗肿瘤的作用[1]

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

Animal Model: SCID mice bearing the MV4;11 xenograft tumors[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.); 5 days a week for 4 weeks
Result: Achieved 92% of tumor growth inhibition at the end of the treatment.
Caused no significant weight loss or other signs of toxicity in mice during the entire experiment.
分子量

824.95

Formula

C44H44N10O5S

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (121.22 mM; 超声助溶; 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 1.2122 mL 6.0610 mL 12.1219 mL
5 mM 0.2424 mL 1.2122 mL 2.4244 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 (protect from light, 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

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 (protect from light, 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2122 mL 6.0610 mL 12.1219 mL 30.3049 mL
5 mM 0.2424 mL 1.2122 mL 2.4244 mL 6.0610 mL
10 mM 0.1212 mL 0.6061 mL 1.2122 mL 3.0305 mL
15 mM 0.0808 mL 0.4041 mL 0.8081 mL 2.0203 mL
20 mM 0.0606 mL 0.3030 mL 0.6061 mL 1.5152 mL
25 mM 0.0485 mL 0.2424 mL 0.4849 mL 1.2122 mL
30 mM 0.0404 mL 0.2020 mL 0.4041 mL 1.0102 mL
40 mM 0.0303 mL 0.1515 mL 0.3030 mL 0.7576 mL
50 mM 0.0242 mL 0.1212 mL 0.2424 mL 0.6061 mL
60 mM 0.0202 mL 0.1010 mL 0.2020 mL 0.5051 mL
80 mM 0.0152 mL 0.0758 mL 0.1515 mL 0.3788 mL
100 mM 0.0121 mL 0.0606 mL 0.1212 mL 0.3030 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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产品名称:
BD-9136
目录号:
HY-149878
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