A-1210477

Name: A-1210477
Brand: MedChemExpress
SKU: HY-12468
Rating: 5.0 (19 reviews)

Cat. No.: HY-12468 Purity: 99.40%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

A-1210477 Chemical Structure

CAS No. : 1668553-26-1

Size	Price	Stock	Quantity
1 mg	USD 33	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 19 publication(s) in Google Scholar

17 Publications Citing Use of MCE A-1210477

: A-1210477 purchased from MedChemExpress. Usage Cited in: Clin Res Hepatol Gas. 2019 Jun;43(3):292-300. [Abstract]; S63845 and A-1210477 trigger apoptosis signaling and reduce the levels of putative stem biomarkers in HCC cell lines.

: 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.

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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

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]
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]
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]

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.

Molecular Weight

850.04

Formula

C₄₆H₅₅N₇O₇S

CAS No.

1668553-26-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.40%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (255 KB) LCMS (276 KB)

Handling Instructions (2659 KB)

References

[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]

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

Complete Stock Solution Preparation Table

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

A-1210477 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:

A-12104771668553-26-1A1210477A 1210477Bcl-2 FamilyApoptosisInhibitorinhibitorinhibit

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A-1210477

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A-1210477 Related Antibodies

17 Publications Citing Use of MCE A-1210477

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References

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A-1210477 Related Antibodies

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Complete Stock Solution Preparation Table

A-1210477 Related Classifications

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