Tapotoclax
Based on 8 publication(s) in Google Scholar
Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a Ki of 0.13 nM.
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- Pureté: 98.35%
- CAS No.: 1883727-34-1
- Formule: C33H41ClN2O5S
- Masse moléculaire:613.21
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tapotoclax
More- Cancer Discov. 2023 Jul 7;13(7):1656-1677. [Abstract]
- Nat Commun. 2025 Aug 21;16(1):7689. [Abstract]
- Sci Adv. 2025 Oct 17;11(42):eadx8662. [Abstract]
- Cell Rep Med. 2024 May 15:101585. [Abstract]
- Biomed Pharmacother. 2023 Dec:168:115738. [Abstract]
- Cell Rep. 2023 Sep 27;42(10):113176. [Abstract]
- Int J Cancer. 2020 Oct 15;147(8):2176-2189. [Abstract]
- EJC Paediatr Oncol. 2024 Jun 3.
Activité biologique
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Mcl-1 0.13 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| OPM-2 | IC50 |
16 nM
Compound: 2; AMG 176
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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
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[PMID: 31736296] |
| OPM-2 | IC50 |
240 nM
Compound: AMG176
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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
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[PMID: 33253879] |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1883727-34-1
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Appearance Solid
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Masse moléculaire 613.21
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Formule C33H41ClN2O5S
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Color White to off-white
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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
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Synonyms
AMG-176
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (8)
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Journal Impact Factor
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Most Recent
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Cancer Discov
2023 Jul 7;13(7):1656-1677. PMID: 37088914 -
Nat Commun
Small round cell sarcoma tumoroid biobank reveals CIC::DUX4 sarcoma vulnerability to MCL-1 inhibition. [Abstract]2025 Aug 21;16(1):7689. PMID: 40841360 -
Sci Adv
Small-molecule OPA1 inhibitors reverse mitochondrial adaptations to overcome therapy resistance in acute myeloid leukemia. [Abstract]2025 Oct 17;11(42):eadx8662. PMID: 41091864 -
Cell Rep Med
Targeting MCL1-driven anti-apoptotic pathways overcomes blast progression after hypomethylating agent failure in chronic myelomonocytic leukemia. [Abstract]2024 May 15:101585. PMID: 38781960 -
Biomed Pharmacother
Combination of MCL-1 and BCL-2 inhibitors is a promising approach for a host-directed therapy for tuberculosis. [Abstract]2023 Dec:168:115738. PMID: 37864894 -
Cell Rep
Targeting MCL-1 triggers DNA damage and an anti-proliferative response independent from apoptosis induction. [Abstract]2023 Sep 27;42(10):113176. PMID: 37773750 -
Int J Cancer
Co-targeting bromodomain and extra-terminal proteins and MCL1 induces synergistic cell death in melanoma. [Abstract]2020 Oct 15;147(8):2176-2189. PMID: 32249419 -
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Caenepeel S, et al. AMG 176, a Selective MCL1 Inhibitor, is Effective in Hematological Cancer Models Alone and in Combination with Established Therapies. Cancer Discov. 2018 Sep 25. pii: CD-18-0387. [Content Brief]
[2]. Garner TP, et al. Progress in targeting the BCL-2 family of proteins. Curr Opin Chem Biol. 2017 Aug;39:133-142. [Content Brief]
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 |
Tapotoclax Related Classifications
HY-101565 Related Classifications
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