2. Apoptosis
  3. Bcl-2 Family Caspase Apoptosis
  4. BRD-810

BRD-810 是一种强效且选择性的 MCL1 抑制剂，Kd 为 0.3 nM。BRD-810 可以特异性阻断 MCL1 的 BH3 结合槽，而对其他抗凋亡蛋白 (如 Bcl-2、Bcl-xL) 几乎没有影响。BRD-810 可有效破坏癌细胞中 MCL1-BAK 复合物 (IC50 = 1.2 nM)，快速激活 Caspase 并诱导细胞凋亡 (apoptosis)。BRD-810 可用于多种血液肿瘤和实体瘤等癌症的研究。

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BRD-810

BRD-810 Chemical Structure

CAS No. : 2329719-65-3

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1 mg ￥11040
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BRD-810 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BRD-810 is a potent and selective MCL1 inhibitor with a Kd of 0.3 nM. BRD-810 can specifically block the BH3 binding groove of MCL1, while having little effect on other anti-apoptotic proteins (such as Bcl-2, Bcl-xL). BRD-810 effectively destroys the MCL1-BAK complex (IC50 = 1.2 nM) in cancer cells, rapidly activates Caspase and induces cell apoptosis. BRD-810 can be used in the research of various cancers such as hematological tumors and solid tumors[1].

IC50 & Target[1]

MCL1

0.3 nM (Kd)

Caspase 3

66 nM (EC50)

体外研究
(In Vitro)

BRD-810 对多种恶性肿瘤和血液系统癌症模型表现出强大的抗增殖活性，包括乳腺癌、肺癌、黑色素瘤、肉瘤、淋巴瘤和白血病，例如 SU-DHL-10 (IC50 = 0.1 nM)、AMO-1 (IC50 = 0.3 nM)、DMS114 (IC50 = 0.6 nM) 和 HCC-1187 (IC50 = 0.9 nM)[1]。
BRD-810 (1 nM-1 μM) 在 HMC1-8 细胞中剂量依赖性地激活 caspase 3 并诱导细胞死亡 (激活 caspase 的 EC50 = 66 nM，抑制细胞生长的 IC50 = 63 nM)[1]。
BRD-810 (0-1 μM，5 分钟-72 小时) 能够在短时间内引发 MCL1 依赖性癌细胞系的不可逆凋亡，但长时间高浓度暴露后，它会对人类诱导多能干细胞衍生的心肌细胞 (hiPS-CM) 表现出显著的心脏毒性[1]。

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

BRD-810 相关抗体:
体内研究
(In Vivo)

BRD-810 (3-50 mg/kg，静脉注射，单剂量或一周一次持续 21-60 天) 无论单独使用还是联合使用，均在各种小鼠血液肿瘤和实体肿瘤模型中表现出强大的抗肿瘤活性，并且在比格犬进行的安全实验中未观察到心脏毒性信号[1]。

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

Animal Model: MOLP-8 cells xenograft models established in 6-8-week-old immunocompromised mice (female CB17/SCID mice[1]
Dosage: 3, 10 and 25 mg/kg
Administration: Intravenous injection (i.v.), single dose or once a week for 30 days
Result: Increased caspase-3.
Dose-dependently inhibited tumor growth.
Animal Model: AMO-1 cells xenograft models established i6–8-week-old immunocompromised mice (female CB17/SCID mice[1]
Dosage: 12.5, 25 and 50 mg/kg
Administration: Intravenous injection (i.v.), single dose
Result: Significantly inhibited tumor growth at 12.5 mg/kg, the dose groups of 25 mg/kg and 50 mg/kg showed stronger effects and could induce complete tumor remission.
Animal Model: BED-810 cells xenograft models established in 6-8-week-old immunocompromised mice (female CB17/SCID mice[1]
Dosage: 25 and 50 mg/kg
Administration: Intravenous injection (i.v.), once a week (25 mg/kg) or every two weeks (50 mg/kg) for 30 days
Result: Effectively inhibited tumor growth and induces tumor regression under both schemes.
Animal Model: SNU398 and A-427 cells xenograft models established in 6-8-week-old immunocompromised mice (female CB17/SCID mice[1]
Dosage: 30 mg/kg
Administration: Intravenous injection (i.v.), twice daily, continue 2 days, with medication discontinued for 5 days for 21 days
Result: Demonstrated comparable anti-tumor efficacy to that of daily administration of Regorafenib (HY-10331) in SNU398 model.
Led to a significant tumor regression, and the effect was significantly better than that of the traditional chemotherapy combination (Cisplatin (HY-17394) + Etoposide (HY-13629)) in A-427 model.
Animal Model: THP-1 cells xenograft models established in 6-8-week-old immunocompromised mice (female CB17/ SCID mice[1]
Dosage: 50 mg/kg with Cytarabine (HY-13605) or Venetoclax (HY-15531)
Administration: Intravenous injection (i.v.), once a week for 60 days
Result: Demonstrated strong individual activity alone and can significantly inhibit tumor growth.
Worked synergistically with Cytarabine or Venetoclax to overcome drug resistance.
Animal Model: Comprehensive assessment of cardiac safety established in purpose-bred, naive beagle dogs (6-9 months old)[1]
Dosage: 3, 8 and 15 mg/kg
Administration: Intravenous injection (i.v.), once a week for 4 weeks
Result: Caused no damage to the microscopic structure of the heart tissue.
Did not interfere with the electrical physiological functions of the heart.
分子量

703.24

Formula

C39H44ClFN4O5
CAS 号
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 : 100 mg/mL (142.20 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 1.4220 mL 7.1099 mL 14.2199 mL
5 mM 0.2844 mL 1.4220 mL 2.8440 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)

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

只
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

BRD-810 相关分类

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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4220 mL 7.1099 mL 14.2199 mL 35.5497 mL
5 mM 0.2844 mL 1.4220 mL 2.8440 mL 7.1099 mL
10 mM 0.1422 mL 0.7110 mL 1.4220 mL 3.5550 mL
15 mM 0.0948 mL 0.4740 mL 0.9480 mL 2.3700 mL
20 mM 0.0711 mL 0.3555 mL 0.7110 mL 1.7775 mL
25 mM 0.0569 mL 0.2844 mL 0.5688 mL 1.4220 mL
30 mM 0.0474 mL 0.2370 mL 0.4740 mL 1.1850 mL
40 mM 0.0355 mL 0.1777 mL 0.3555 mL 0.8887 mL
50 mM 0.0284 mL 0.1422 mL 0.2844 mL 0.7110 mL
60 mM 0.0237 mL 0.1185 mL 0.2370 mL 0.5925 mL
80 mM 0.0178 mL 0.0889 mL 0.1777 mL 0.4444 mL
100 mM 0.0142 mL 0.0711 mL 0.1422 mL 0.3555 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.

Keywords:

BRD-8102329719-65-3BRD810BRD 810Bcl-2 FamilyCaspaseApoptosisMCL1BH3caspaseblood cancersolid tumorInhibitorinhibitorinhibit

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