Art. -Nr.: HY-12468

A-1210477

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

A-1210477 is a potent and selective inhibitor of MCL-1 with a K_i of 0.45 nM. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.

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Reinheit: 99.86%
CAS. Nr.: 1668553-26-1
Formel: C₄₆H₅₅N₇O₇S
Molecular Weight:850.04

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

A-1210477 Chemical Structure

CAS. Nr.: 1668553-26-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

A-1210477 is a potent and selective inhibitor of MCL-1 with a K_i of 0.45 nM^[1]. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner^[2].

IC₅₀ & Target^[1]

Mcl-1

0.45 nM (Ki)

Bcl-2

132 nM (Ki)

Bfl-1

660 nM (Ki)

Bcl-W

2280 nM (Ki)

Apoptosis

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	>20 μM Compound: A1210477	Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
HeLa	IC₅₀	>20 μM Compound: A1210477	Cytotoxicity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
HL-60	IC₅₀	2.46 μM Compound: A1210477	Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
HL-60	IC₅₀	5.53 μM Compound: A-1210477	Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 39121336]
K562	IC₅₀	>30 μM Compound: 4; A1210477	Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
K562	IC₅₀	13.9 μM Compound: A-1210477	Cytotoxicity against human K562 cells after 24 hrs by MTT assay Cytotoxicity against human K562 cells after 24 hrs by MTT assay	[PMID: 32794745]
KMS-12-PE	IC₅₀	>40 μM Compound: A-1210477	Cytotoxicity against human KMS-12-PE cells after 24 hrs by MTT assay Cytotoxicity against human KMS-12-PE cells after 24 hrs by MTT assay	[PMID: 32794745]
L-363	IC₅₀	11.8 μM Compound: A-1210477	Cytotoxicity against human L-363 cells after 24 hrs by MTT assay Cytotoxicity against human L-363 cells after 24 hrs by MTT assay	[PMID: 32794745]
LP-1	IC₅₀	10.6 μM Compound: A-1210477	Cytotoxicity against human LP-1 cells after 24 hrs by MTT assay Cytotoxicity against human LP-1 cells after 24 hrs by MTT assay	[PMID: 32794745]
MM1.S	IC₅₀	>40 μM Compound: A-1210477	Cytotoxicity against human MM1.S cells after 24 hrs by MTT assay Cytotoxicity against human MM1.S cells after 24 hrs by MTT assay	[PMID: 32794745]
MOLM-13	IC₅₀	8.15 μM Compound: A-1210477	Antiproliferative activity against human MOLM-13 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human MOLM-13 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 39121336]
MOLP-8	IC₅₀	9.7 μM Compound: A-1210477	Cytotoxicity against human MOLP8 cells after 24 hrs by MTT assay Cytotoxicity against human MOLP8 cells after 24 hrs by MTT assay	[PMID: 32794745]
MV4-11	IC₅₀	1.55 μM Compound: 4; A1210477	Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H23	IC₅₀	13.5 μM Compound: 4; A1210477	Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H929	IC₅₀	0.9 μM Compound: 4; A1210477	Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H929	IC₅₀	8.6 μM Compound: A-1210477	Cytotoxicity against human NCI-H929 cells after 24 hrs by MTT assay Cytotoxicity against human NCI-H929 cells after 24 hrs by MTT assay	[PMID: 32794745]
RS4-11	IC₅₀	7.31 μM Compound: A1210477	Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
SK-BR-3	IC₅₀	4.31 μM Compound: 4; A1210477	Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
THP-1	IC₅₀	5.65 μM Compound: A-1210477	Antiproliferative activity against human THP-1 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human THP-1 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 39121336]
U-937	IC₅₀	4.71 μM Compound: A-1210477	Antiproliferative activity against human U-937 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay Antiproliferative activity against human U-937 cells assessed as growth inhibition measured after 72 hrs by CCK-8 assay	[PMID: 39121336]

In Vitro

A-1210477 (10 μM) reduces the amount of BIM co-immunoprecipitated with MCL-1 antibody, and triggers MCL-1 elevation in a variety of cancer cell lines, including the breast cancer cell line HCC-1806. A-1210477 inhibits MCL-1-NOXA interactions with an IC₅₀ of approximately 1 μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions. The NSCLC cell lines H2110 and H23 are sensitive to A-1210477 with cell viability IC₅₀<10 μM, confirming that A-1210477 can kill MCL-1-dependent cell lines^[1].

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

Chemical Information

CAS. Nr. 1668553-26-1
Appearance Solid
Molecular Weight 850.04
Formel C₄₆H₅₅N₇O₇S
Color White to off-white
SMILES

O=C(C(N1CCN2CCOCC2)=C(CCCOC3=C4C=CC=CC4=CC=C3)C5=C1C(C6=C(COC7=CC=C(N8CCN(S(=O)(N(C)C)=O)CC8)C=C7)N(C)N=C6C)=CC=C5)O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (20)

All WB

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Small round cell sarcoma tumoroid biobank reveals CIC::DUX4 sarcoma vulnerability to MCL-1 inhibition. [Abstract]

2025 Aug 21;16(1):7689. PMID: 40841360
Cell Death Differ

DNase II activated by the mitochondrial apoptotic pathway regulates RIP1-dependent non-apoptotic hepatocyte death via the TLR9/IFN-β signaling pathway. [Abstract]

2019 Mar;26(3):470-486. PMID: 29855540
Cell Death Dis

Constitutive BAK/MCL1 complexes predict paclitaxel and S63845 sensitivity of ovarian cancer. [Abstract]

2021 Aug 12;12(8):789. PMID: 34385422
Cell Death Dis

A small natural molecule CADPE kills residual colorectal cancer cells by inhibiting key transcription factors and translation initiation factors. [Abstract]

2020 Nov 15;11(11):982. PMID: 33191401
Aging Cell

Morphofunctional Heterogeneity and Plasticity of Glioblastoma Cells Induced to Senescence by Temozolomide. [Abstract]

2026 Apr;25(4):e70477. PMID: 41963773
J Pineal Res

2024 Jan 31.
JCI Insight

OGDH and Bcl-xL loss causes synthetic lethality in glioblastoma. [Abstract]

2024 Mar 14;9(8):e172565. PMID: 38483541
Biochem Pharmacol

Hydroquinone destabilizes BIM mRNA through upregulation of p62 in chronic myeloid leukemia cells. [Abstract]

2022 May;199:115017. PMID: 35346662
Int J Mol Sci

Albendazole-Induced SIRT3 Upregulation Protects Human Leukemia K562 Cells from the Cytotoxicity of MCL1 Suppression. [Abstract]

2020 May 30;21(11):3907. PMID: 32486166
Chem Biol Interact

BCL2 inhibitor ABT-199 and BCL2L1 inhibitor WEHI-539 coordinately promote NOXA-mediated degradation of MCL1 in human leukemia cells. [Abstract]

2022 Jul 1;361:109978. PMID: 35561756
Sci Rep

Matrix Metalloproteinase Expressions Play Important role in Prediction of Ovarian Cancer Outcome. [Abstract]

2019 Aug 12;9(1):11677. PMID: 31406154
J Cell Physiol

NOXA-mediated degradation of MCL1 and BCL2L1 causes apoptosis of daunorubicin-treated human acute myeloid leukemia cells. [Abstract]

2021 Nov;236(11):7356-7375. PMID: 33982799
Open Biol

Inhibition of Bcl-xL sensitizes cells to mitotic blockers, but not mitotic drivers. [Abstract]

2016 Aug;6(8). pii: 160134. PMID: 27512141

A-1210477 purchased from MedChemExpress. Usage Cited in: Open Biol. 2016 Aug;6(8). pii: 160134. [Abstract]

Immunoblots showing affinity purification of GFP-tagged Mcl-1 in the presence of 2 μM A-1210477, and detection of co-purifying Bak.
J Cell Biochem

Mcl-1 is a Gatekeeper Molecule to Regulate the Crosstalk Between Ferroptotic Agent-Induced ER Stress and TRAIL-Induced Apoptosis. [Abstract]

2025 Jan;126(1):e30681. PMID: 39853862
Clin Res Hepatol Gastroenterol

Targeting Mcl-1 inhibits survival and self-renewal of hepatocellular cancer stem-like cells. [Abstract]

2019 Jun;43(3):292-300. PMID: 30528319
Oncol Lett

A-1210477, a selective MCL-1 inhibitor, overcomes ABT-737 resistance in AML. [Abstract]

2019 Nov;18(5):5481-5489. PMID: 31612056
Leuk Lymphoma

MCL-1 or BCL-xL-dependent resistance to the BCL-2 antagonist (ABT-199) can be overcome by specific inhibitor as single agents and in combination with ABT-199 in acute myeloid leukemia cells. [Abstract]

2019 Sep;60(9):2170-2180. PMID: 30626241
Res Sq

2024 Aug 04.
bioRxiv

2023 Aug 5.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 10 mg/mL (11.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1764 mL

5.8821 mL

11.7642 mL

5 mM

0.2353 mL

1.1764 mL

2.3528 mL

10 mM

0.1176 mL

0.5882 mL

1.1764 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (1.18 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 1 mg/mL (1.18 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (1.18 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

TR-FRET-binding affinity assays are performed for BCL-2, BCL-XL, and MCL-1 in 4.52 mM monobasic potassium phosphate, 15.48 mM dibasic potassium phosphate, 1 mM sodium EDTA, 0.05% Pluronic F-68 detergent, 50 mM sodium chloride, and 1 mM DTT (pH 7.5) for BCL-XL.6 For MCL-1 assays, GST-tagged MCL-1 (1 nM) is mixed with 100 nM f-Bak, 1 nM Tb-labeled anti-GST antibody, and compound at room temperature (RT) for 60 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-GST antibody) emission filters.

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

Cell Assay^[1]

Adherent cell lines are seeded at 50 000 cells per well in 96-well plates and treated for 48 h with compounds diluted in half-log steps starting at 30 μM and ending at 0.001 μM. Multiple myeloma cell lines are seeded at 15 000-20 000 cells per well and treated similarly. Effects on proliferation and viability are determined using CellTiter-Glo reagent from Promega according to the manufacturer's instructions. IC₅₀ values are determined by non-linear regression analysis of the concentration response data.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Leverson JD, et al. Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax). Cell Death Dis. 2015 Jan 15;6:e1590. [Content Brief]

[2]. Qing Wang, et al. A-1210477, a selective MCL-1 inhibitor, overcomes ABT-737 resistance in AML. Oncol Lett. 2019 Nov;18(5):5481-5489. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1764 mL	5.8821 mL	11.7642 mL	29.4104 mL
	5 mM	0.2353 mL	1.1764 mL	2.3528 mL	5.8821 mL
	10 mM	0.1176 mL	0.5882 mL	1.1764 mL	2.9410 mL

Keywords

A-1210477

20 Cited Publications

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A-1210477

Apoptosis Compound Library

Anti-Cancer Compound Library

Chemical Probe Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) A-1210477

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

A-1210477

Apoptosis Compound Library

Anti-Cancer Compound Library

Chemical Probe Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) A-1210477

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

A-1210477 Related Classifications

HY-12468 Related Classifications