2. Apoptosis
  3. Bcl-2 Family
  4. Mcl-1 inhibitor 3

Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.
.

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

Mcl-1 inhibitor 3 Chemical Structure

Mcl-1 inhibitor 3 Chemical Structure

CAS No. : 2376774-73-9

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Mcl-1 inhibitor 3 Related Antibodies

Top Publications Citing Use of Products

View All Bcl-2 Family Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity[1].
.

IC50 & Target

Mcl-1

19 nM (IC50)

Mcl-1

0.061 nM (Ki)

In Vitro

Mcl-1 inhibitor 3 shows an IC50 value of 19 nM in an OPM-2 cell viability assay, and a Ki value of 0.061 nM in Mcl-1 HTRF/TR-FRET assay[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Mcl-1 inhibitor 3 Related Antibodies
In Vivo

Mcl-1 inhibitor 3 (oral administration; 3, 10, or 30 mg/kg; 6 hours) causes a significant loss of luminescence (∼40%) over vehicle at 30 mg/kg,This effect was observed with unbound drug levels in plasma, the [plasma]u/OPM-2 IC50 values are 0.24, 0.93 and 3.65 μM in 3, 10, 30 mg/kg doses,respectively[1].
Mcl-1 inhibitor 3 (oral administration; 10, 30, or 60 mg/kg; 6 hours) activates Bak by 8-fold at 30 mg/kg and by 14-fold at 60 mg/kg in this OPM-2 Luc assay,this test is based on the detection of activated Bak in nude mice subcutaneously injected with via electrochemiluminescence.[1].
Mcl-1 inhibitor 3 (oral administration; 10, 30, or 60 mg/kg; 30 days) led to a robust dose-dependent tumor growth inhibition at 30 mg/kg (44% TGI) and 34% tumor regression when the animals were dosed at 60 mg/kg.Lastly, no body weight loss is observed in any of the mice in this study efficacy models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude miceinjected with HEK293 cells[1]
Dosage: 3, 10, or 30 mg/kg
Administration: Oral administration
Result: Showed a disruption of the Mcl-1/Bak interaction in this in vivo model.
Animal Model: Nude mice injected with human OPM-2 multiple myeloma tumor cells[1]
Dosage: 10, 30, or 60 mg/kg
Administration: Oral administration
Result: Exhibited a inhibition of tumor growth without any toxicity.
Molecular Weight

820.38

Formula

C40H52ClF2N5O7S
CAS No.
SMILES

ClC1=CC(CCC2)=C(C=C1)[C@]2(CO3)CN(C[C@H]4[C@@H](CC4)[C@@H](OCCN5CC(F)(F)C5)/C=C/CCN(C)C6=O)C7=C3C=CC([C@@](O)(C(NS(=O)(N(C)C)=O)=O)C6)=C7
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Mcl-1 inhibitor 3 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

Mcl-1 inhibitor 32376774-73-9Bcl-2 FamilyMyeloma cancer,Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Mcl-1 inhibitor 3
Cat. No.:
HY-133015
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.