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

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.

For research use only. We do not sell to patients.

BRD-810

BRD-810 Chemical Structure

CAS No. : 2329719-65-3

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Based on 1 publication(s) in Google Scholar

BRD-810 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

In Vitro

BRD-810 exhibits strong antiproliferative activity against range of strong and hematological cancer models, including breast cancer, lung cancer, melanoma, sarcoma, lymphoma and leukemia, such as SU-DHL-10 (IC50 = 0.1 nM), AMO-1 (IC50 = 0.3 nM), DMS114 (IC50 = 0.6 nM) and HCC-1187 (IC50 = 0.9 nM)[1].
BRD-810 (1 nM-1 μM) leads to the activation of caspase 3 and induction of cell death dose dependently in HMC1-8 cells (EC50 = 66 nM for caspase activation and IC50 = 63 nM for cell growth inhibition)[1].
BRD-810 (0-1 μM, 5 min-72 h) is capable of triggering irreversible apoptosis in MCL1-dependent cancer cell lines within a short period of time, but after prolonged exposure at high concentrations, it shows significant cardiotoxicity to human induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs)[1].

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

BRD-810 Related Antibodies
In Vivo

BRD-810 (3-50 mg/kg, i.v., single dose or once a week for 21-60 days) demonstrates strong anti-tumor activity in various mouse models of hematological and solid tumors whether used alone or in combination, and no cardiac toxicity signals are observed in the safety experiments conducted in dogs[1].

MedChemExpress (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.
Molecular Weight

703.24

Formula

C39H44ClFN4O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C(N1CCCCO[C@H](CCN2CCOCC2)C3=NN(C)C(CC)=C43)=C(CCCOC5=C6C(C=C(F)C=C6)=CC=C5)C7=C1C4=C(Cl)C=C7
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (142.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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BRD-810 Related Classifications

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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