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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

🥰Excellent

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	BCL-W:>10 μM (Kd), BCL2A1:>10 μM (Kd), Bfl-1:1.57 μM (Ki), Bcl-2:10 μM (Ki), MCL1:0.23 nM (Kd), BCL-XL:>10 μM (Kd), MCL1:0.02 μM (Ki), Bcl-2:>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
Color	White
Appearance	Solid

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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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