2. Apoptosis
  3. Bcl-2 Family
  4. Tapotoclax

Tapotoclax  (Synonyms: AMG-176)

Cat. No.: HY-101565 Purity: 99.18%
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AMG-176 est un inhibiteur de MCL-1 qui est puissant, sélectif et oralement actif avec un Ki de 0,13 nM.

Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a Ki of 0.13 nM.

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

Tapotoclax Chemical Structure

Tapotoclax Chemical Structure

CAS No. : 1883727-34-1

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1 mg USD 680 In-stock
5 mg USD 1950 In-stock
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Based on 5 publication(s) in Google Scholar

Tapotoclax 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

Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a Ki of 0.13 nM[1][2].

IC50 & Target[1]

Mcl-1

0.13 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
OPM-2 IC50
16 nM
Compound: 2; AMG 176
Antiproliferative activity against human OPM2 cells assessed as reduction in cell viability after 16 hrs by CellTiter-Glo based luminescence assay
Antiproliferative activity against human OPM2 cells assessed as reduction in cell viability after 16 hrs by CellTiter-Glo based luminescence assay
[PMID: 31736296]
OPM-2 IC50
240 nM
Compound: AMG176
Anticancer activity against human OPM-2 cells assessed as inhibition of cell viability incubated for 24 hrs in presence of 10% FBS by Cell-titer Glo assay
Anticancer activity against human OPM-2 cells assessed as inhibition of cell viability incubated for 24 hrs in presence of 10% FBS by Cell-titer Glo assay
[PMID: 33253879]
In Vitro

Tapotoclax is an inhibitor of induced myeloid leukemia cell differentiation protein MCL-1 (Ki=0.13 nM), with potential pro-apoptotic and antineoplastic activities. Upon administration, Tapotoclax binds to and inhibits the activity of MCL-1. This disrupts the formation of MCL-1/Bcl-2-like protein 11 (BCL2L11; BIM) complexes and induces apoptosis in tumor cells[1][2].

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

Tapotoclax Related Antibodies
Clinical Trial
Molecular Weight

613.21

Formula

C33H41ClN2O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C2C(CCC[C@@]23CN(C[C@@](CC4)([H])[C@]4([H])[C@H](/C=C/C[C@H](C)[C@H]5C)OC)C6=CC(C(NS5(=O)=O)=O)=CC=C6OC3)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (101.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6308 mL 8.1538 mL 16.3076 mL
5 mM 0.3262 mL 1.6308 mL 3.2615 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2 mg/mL (3.26 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2 mg/mL (3.26 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.53%

SDS (252 KB)

COA (259 KB) LCMS (141 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6308 mL 8.1538 mL 16.3076 mL 40.7691 mL
5 mM 0.3262 mL 1.6308 mL 3.2615 mL 8.1538 mL
10 mM 0.1631 mL 0.8154 mL 1.6308 mL 4.0769 mL
15 mM 0.1087 mL 0.5436 mL 1.0872 mL 2.7179 mL
20 mM 0.0815 mL 0.4077 mL 0.8154 mL 2.0385 mL
25 mM 0.0652 mL 0.3262 mL 0.6523 mL 1.6308 mL
30 mM 0.0544 mL 0.2718 mL 0.5436 mL 1.3590 mL
40 mM 0.0408 mL 0.2038 mL 0.4077 mL 1.0192 mL
50 mM 0.0326 mL 0.1631 mL 0.3262 mL 0.8154 mL
60 mM 0.0272 mL 0.1359 mL 0.2718 mL 0.6795 mL
80 mM 0.0204 mL 0.1019 mL 0.2038 mL 0.5096 mL
100 mM 0.0163 mL 0.0815 mL 0.1631 mL 0.4077 mL
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Tapotoclax Related Classifications

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:

Tapotoclax1883727-34-1AMG-176AMG176AMG 176Bcl-2 FamilyInhibitorinhibitorinhibit

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