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Purity: ≥98%
AMG-176 (AMG176; tapotoclax) is a novel, potent, selective and orally bioavailable inhibitor of MCL-1 (myeloid cell leukemia-1) with a Ki of 0.13 nM. Potential pro-apoptotic and anti-cancer effects of AMG-176 exist. MCL-1 is bound by AMG 176, which then stops it from working. This causes apoptosis in tumor cells and interferes with the formation of MCL-1/Bcl-2-like protein 11 (BCL2L11; BIM) complexes. The Bcl-2 family of proteins member MCL-1, an anti-apoptotic protein, is upregulated in cancer cells and supports the survival of tumor cells.
| Targets |
Mcl-1 (Ki = 0.13 nM)
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|---|---|
| ln Vitro |
Tapoclax is a compound that has the ability to stimulate cell color development and anti-tumor action. It also promotes the production of MCL-1 (Ki=0.13 nM) in inducible myeloid leukemia cells. After then, tapotoclax attaches to MCL-1 and prevents its function. It stimulates tumor cells and interferes with the formation of the MCL-1/Bcl-2-like protein 11 (BCL2L11; BIM) complex [1][2].
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| References | |
| Additional Infomation |
Tapotoclax is an inhibitor of induced myeloid leukemia cell differentiation protein MCL-1 (myeloid cell leukemia-1), 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. MCL-1, an anti-apoptotic protein belonging to the Bcl-2 family of proteins, is upregulated in cancer cells and promotes tumor cell survival.
Drug Indication Treatment of acute myeloid leukaemia |
| Molecular Formula |
C33H41CLN2O5S
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|---|---|
| Molecular Weight |
613.207047224045
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| Exact Mass |
612.24
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| Elemental Analysis |
C, 64.64; H, 6.74; Cl, 5.78; N, 4.57; O, 13.05; S, 5.23
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| CAS # |
1883727-34-1
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| Related CAS # |
1883727-34-1
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| PubChem CID |
118910268
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| Appearance |
White to off-white solid powder
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| LogP |
6.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
42
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| Complexity |
1110
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@H]1C/C=C/[C@@H]([C@@H]2CC[C@H]2CN3C[C@@]4(CCCC5=C4C=CC(=C5)Cl)COC6=C3C=C(C=C6)C(=O)NS(=O)(=O)[C@@H]1C)OC
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| InChi Key |
JQNINBDKGLWYMU-GEAQBIRJSA-N
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| InChi Code |
InChI=1S/C33H41ClN2O5S/c1-21-6-4-8-30(40-3)27-12-9-25(27)18-36-19-33(15-5-7-23-16-26(34)11-13-28(23)33)20-41-31-14-10-24(17-29(31)36)32(37)35-42(38,39)22(21)2/h4,8,10-11,13-14,16-17,21-22,25,27,30H,5-7,9,12,15,18-20H2,1-3H3,(H,35,37)/b8-4+/t21-,22+,25-,27+,30-,33-/m0/s1
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| Chemical Name |
(3'R,4S,6'R,7'S,8'E,11'S,12'R)-7-chloro-7'-methoxy-11',12'-dimethyl-13',13'-dioxospiro[2,3-dihydro-1H-naphthalene-4,22'-20-oxa-13lambda6-thia-1,14-diazatetracyclo[14.7.2.03,6.019,24]pentacosa-8,16(25),17,19(24)-tetraene]-15'-one
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| Synonyms |
tapotoclaxum; tapotoclax; AMG-176; AMG176; AMG 176
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~62.5 mg/mL (~101.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (3.26 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2 mg/mL (3.26 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2 mg/mL (3.26 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1631 mL | 0.8154 mL | 1.6308 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05209152 | Recruiting | Drug: AMG 176 Drug: Azacitidine |
Higher Risk Myelodysplastic Syndrome Chronic Myelomonocytic Leukemia |
Amgen | September 1, 2019 | Phase 1 |
| NCT02675452 | Recruiting | Drug: AMG 176 Drug: Azacitidine |
Relapsed or Refractory Multiple Myeloma Relapsed or Refractory Acute Myeloid Leukemia |
Amgen | June 13, 2016 | Phase 1 |
| NCT03797261 | Terminated | Drug: Venetoclax Drug: AMG 176 |
Acute Myeloid Leukemia Non-Hodgkin's Lymphoma |
AbbVie | March 18, 2019 | Phase 1 |
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