Name: A-1210477
Brand: Selleck Chemicals
SKU: S7790
Availability: InStock
Rating: 5 (50 reviews)

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Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Other Bcl-2 Inhibitors	Navitoclax (ABT-263) S63845 ABT-737 Obatoclax Mesylate (GX15-070) A-1331852 TW-37 A-1155463 Dihydrochloride AZD5991 UMI-77 (R)-(-)-Gossypol (AT-101) acetic acid

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
human H23 cells	Cytotoxicity assay		24 hrs		Cytotoxicity against human H23 cells incubated for 24 hrs by CCK8 assay	31389699
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 3 mg/mL (3.52 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.150mg/ml (0.18mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.150mg/ml (0.18mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	850.04	Formula	C₄₆H₅₅N₇O₇S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1668553-26-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=NN(C(=C1C2=CC=CC3=C2N(C(=C3CCCOC4=CC=CC5=CC=CC=C54)C(=O)O)CCN6CCOCC6)COC7=CC=C(C=C7)N8CCN(CC8)S(=O)(=O)N(C)C)C

Mechanism of Action

Targets/IC₅₀/Ki	MCL-1 (Cell-free assay) 26.2 nM
In vitro	In H929 cells, A-1210477 binds to MCL-1 with high affinity and induces MCL-1 protein elevation. In H929, H2110, and H23 cells, this compound induces the hallmarks of apoptosis, and inhibits MCL-1-dependent cell viability. It also synergizes with navitoclax to kill a variety of cancer cell lines. In SKBR3 cells, this chemical inhibits MCL-1–BIM interaction and induces classical features of apoptosis. In addition, it sensitizes non-Hodgkin's lymphoma cell lines to venetoclax (ABT-199).
Kinase Assay	Binding affinity assays
Kinase Assay	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 MCL-1 assays, GST-tagged MCL-1 (1 nM) is mixed with 100 nM f-Bak, 1 nM Tb-labeled anti-GST antibody, and this 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25590800/ [2] https://pubmed.ncbi.nlm.nih.gov/26013319/ [3] https://pubmed.ncbi.nlm.nih.gov/26565405/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pERK / ERK / p-MCL1 / Caspase-3 PARP / MEK / Cyt c/ Tom20 Mcl-1		27765849

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A-1210477 Bcl-2 inhibitor

Chemical Structure

Molecular Weight: 850.04