OP-3136
Based on 1 Customer Validation
OP-3136 is an orally active, highly selective inhibitor of KAT6A and KAT6B. OP-3136 inhibits the proliferation of prostate cancer, ovarian cancer and non-small cell lung cancer cells that express or overexpress KAT6A. OP-3136 reduces the proliferative capacity of cancer cells and suppresses cell growth in ER+ breast cancer cell models with KAT6 overexpression. OP-3136 induces tumor regression and inhibits tumor growth in an ovarian cancer xenograft model in immunodeficient mice. OP-3136 inhibits tumor growth in a non-small cell lung cancer xenograft model in immunodeficient mice. OP-3136 can be used in research related to HR+/HER2- breast cancer, prostate cancer, ovarian cancer and non-small cell lung cancer (NSCLC).
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 3056105-63-3
- Formula: C20H22N4O7S
- Molecular Weight:462.48
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Storage:
-80°C
Biological Activity
|
KAT6A |
KAT6B |
OP-3136 inhibits proliferation of VCAP, OAW28, OVCAR3, and LCLC-97TM1 cell lines[1].
OP-3136 reduces the proliferation of breast cancer cell lines and inhibits growth in KAT6-overexpressing ER+ breast cancer cell models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
OP-3136 (1 mg/kg; p.o.) monotherapy inhibits tumor growth in LCLC-97TM1 NSCLC xenografts with a TGI of 62% at a dose of 1 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3056105-63-3
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Appearance Solid
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Molecular Weight 462.48
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Formula C20H22N4O7S
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Color White to off-white
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SMILES
COC1=CC(OC)=C(C(OC)=C1)S(=O)(NC(C2=NC(OC)=C(C=C2)CN3C=CC=N3)=O)=O
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Shipping
Shipping with dry ice.
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Storage
-80°C
Solvent & Solubility
DMSO : 25 mg/mL (54.06 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, 6 months. When stored at -80°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, 6 months. When stored at -80°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 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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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, 6 months. When stored at -80°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1623 mL | 10.8113 mL | 21.6226 mL | 54.0564 mL |
| 5 mM | 0.4325 mL | 2.1623 mL | 4.3245 mL | 10.8113 mL | |
| 10 mM | 0.2162 mL | 1.0811 mL | 2.1623 mL | 5.4056 mL | |
| 15 mM | 0.1442 mL | 0.7208 mL | 1.4415 mL | 3.6038 mL | |
| 20 mM | 0.1081 mL | 0.5406 mL | 1.0811 mL | 2.7028 mL | |
| 25 mM | 0.0865 mL | 0.4325 mL | 0.8649 mL | 2.1623 mL | |
| 30 mM | 0.0721 mL | 0.3604 mL | 0.7208 mL | 1.8019 mL | |
| 40 mM | 0.0541 mL | 0.2703 mL | 0.5406 mL | 1.3514 mL | |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4325 mL | 1.0811 mL |