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Mcl-1 inhibitor 6

Name: Mcl-1 inhibitor 6
Brand: TargetMol
SKU: T40230
Rating: 4.5 (1 reviews)

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Catalog No. T40230Cas No. 2598978-56-2

Mcl-1 inhibitor 6 is a potent, orally active small molecule that selectively targets the anti-apoptotic protein myeloid cell leukemia 1 (Mcl-1). Mcl-1 inhibitor 6 binds with high affinity, with a dissociation constant (K d) of 0.23 nM, and exhibits binding activity with a K i of 0.02 μM. Mcl-1 inhibitor 6 displays exceptional selectivity over other anti-apoptotic Bcl-2 family proteins, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, all of which display binding constants greater than 10 μM. Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity in preclinical models, highlighting its potential as a therapeutic candidate in oncology.

Mcl-1 inhibitor 6

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Catalog No. T40230Cas No. 2598978-56-2

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Product Introduction

Bioactivity

Description	Mcl-1 inhibitor 6 is a potent, orally active small molecule that selectively targets the anti-apoptotic protein myeloid cell leukemia 1 (Mcl-1). Mcl-1 inhibitor 6 binds with high affinity, with a dissociation constant (K d) of 0.23 nM, and exhibits binding activity with a K i of 0.02 μM. Mcl-1 inhibitor 6 displays exceptional selectivity over other anti-apoptotic Bcl-2 family proteins, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, all of which display binding constants greater than 10 μM. Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity in preclinical models, highlighting its potential as a therapeutic candidate in oncology.
Targets&IC50	BCL2A1:>10 μM (Kd), BCL-W:>10 μM (Kd), Bfl-1:1.57 μM (Ki), Bcl-2:10 μM (Ki), Bcl-2:>10 μM (Kd), MCL1:0.02 μM (Ki), MCL1:0.23 nM (Kd), BCL-XL:>10 μM (Kd)
In vitro	Methods: H929 cells were treated with Mcl-1 inhibitor 6 (0.1, 5 μM, 4 h), and the expression of related proteins was analyzed by Western Blot. Results: After treatment with Mcl-1 inhibitor 6, PARP cleavage was significantly upregulated in a concentration-dependent manner. [1]
In vivo	Methods: Mcl-1 inhibitor 6 (20, 60 mg/kg, administered every 2 days for 14 days) was administered to Balb/c nude mice bearing MV4-11 xenograft tumors via intraperitoneal injection or oral gavage to investigate the antitumor activity of Mcl-1 inhibitor 6. Results: Mcl-1 inhibitor 6 demonstrated significant tumor growth inhibition in vivo. [1]

Chemical Properties

Molecular Weight	518.02
Formula	C₂₆H₂₈ClNO₆S
Cas No.	2598978-56-2
Smiles	O=C(O)C1=C(C(=C(N1CCCOC=2C=C(C(Cl)=C(C2)C)C)C)S(=O)(=O)C3=CC=C(C=C3)C(=O)C)C

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (154.43 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9304 mL	9.6521 mL	19.3043 mL	96.5214 mL
5 mM	0.3861 mL	1.9304 mL	3.8609 mL	19.3043 mL
10 mM	0.1930 mL	0.9652 mL	1.9304 mL	9.6521 mL
20 mM	0.0965 mL	0.4826 mL	0.9652 mL	4.8261 mL
50 mM	0.0386 mL	0.1930 mL	0.3861 mL	1.9304 mL
100 mM	0.0193 mL	0.0965 mL	0.1930 mL	0.9652 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc