Home Tools
Log in
Cart

Mcl-1 inhibitor 6

Catalog No. T40230   CAS 2598978-56-2

Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compound exhibits exceptional selectivity over other members of the Bcl-2 family, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w (K d <10 μM). Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Mcl-1 inhibitor 6 Chemical Structure
Mcl-1 inhibitor 6, CAS 2598978-56-2
Please contact us for prices and availability for the specification of product you are interested at.
Product consultation
Get quote
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compound exhibits exceptional selectivity over other members of the Bcl-2 family, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w (K d >10 μM). Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity.
Targets&IC50 Bcl2A1:>10 μM (Kd), Bcl-W:>10 μM (Kd), Bcl-xL:>10 μM (Kd), Bcl-2:>10 μM (Kd), Bcl-2:10 μM (Ki), Bfl-1:1.57 μM (Ki), MCL-1:0.02 μM (Ki), MCL-1:0.23 nM (Kd)
In vitro Mcl-1 inhibitor 6 has K i s of 10 μM and 1.57μM for Bcl-2 and Bfl-1, respectively[1]. Mcl-1 inhibitor 6 (1, 5 μM; for 48 h) significantly induces apoptosis in a concentration-dependent manner[1]. Mcl-1 inhibitor 6 (0.1, 5 μM; for 4 h) remarkably upregulates PARP cleavage in H929 cells in a concentration-dependent manner[1]. Mcl-1 inhibitor 6 (for 72 h) shows antiproliferative activities against the tumor cell lines (H929, MV4-11, SK-BR-3, NCI-H23; IC 50 =0.36-3.02 μM). Mcl-1 inhibitor 6 shows ideal selectivity against CML cell line K562 (IC 50 >30 μM)[1]. Apoptosis Analysis[1]Cell Line: H929 cells Concentration: 1, 5 μM Incubation Time: For 48 hours Result: Significantly induced apoptosis in a concentration-dependent manner. Western Blot Analysis[1]Cell Line: H929 cells Concentration: 0.1, 0.5, 1, 5 μM Incubation Time: For 4 hours Result: Remarkably upregulated PARP cleavage in H929 cells in a concentration-dependent manner.
In vivo Mcl-1 inhibitor 6 (compound 40; 60 mg/kg with PO or 20 mg/kg with IP; every two days for 14 days) shows desired in vivo tumor growth inhibition activity[1]. Mcl-1 inhibitor 6 (3 mg/kg with IV or 10 mg/kg with PO) has a T 1/2 of 2.3 hours, a CL of 15.18 mL/min?kg by IV[1]. Animal Model: Balb/c nude female mice (7 weeks) loaded with MV4-11 xenografts[1]Dosage: 60 mg/kg (PO) or 20 mg/kg (IP) Administration: IP or PO; every two days for 14 days Result: Showed desired in vivo tumor growth inhibition activity (T/C = 37.30% and 5.52% by po and ip administration, respectively). Animal Model: SD rats (200-250 g)[1]Dosage: 3 mg/kg (IV) or 10 mg/kg (PO) (Pharmacokinetic Analysis) Administration: IV or PO Result: Had a T 1/2 of 2.3 hours, a CL of 15.18 mL/min?kg by IV. Had a T 1/2 of 2.1 hours, a CL of 36.8 mL/min?kg and a C max of 2012.95 ng/mL.
Molecular Weight 518.02
Formula C26H28ClNO6S
CAS No. 2598978-56-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Peng-Ju Zhu, et al. Discovery of 3,5-Dimethyl-4-Sulfonyl-1 H-Pyrrole-Based Myeloid Cell Leukemia 1 Inhibitors with High Affinity, Selectivity, and Oral Bioavailability. J Med Chem. 2021 Aug 12;64(15):11330-11353.

TargetMolDose Conversion

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

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

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.

Keywords

Mcl-1 inhibitor 6 2598978-56-2 Mcl1 inhibitor 6 Mcl 1 inhibitor 6 inhibitor inhibit

 

TargetMol