TH9028
TH9028 is an inhibitor of MTHFD1, MTHFD2 and MTHFD2L, with IC50 values of 0.5 nM, 11 nM and 27 nM, respectively. TH9028 reduces replication fork speed, induces replication stress, triggers S-phase arrest, initiates apoptosis, impairs thymidine production, and causes erroneous uracil incorporation into DNA. TH9028 can be used in research related to acute myeloid leukemia.
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- No. CAS: 2379556-15-5
- Fòrmula: C16H18N12O5
- Peso molecular:458.39
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
|
13169 11 nM (IC50) |
13168 7.97 nM (IC50) |
13170 27 nM (IC50) |
13171 0.5 nM (IC50) |
TH9028 (10-10 to 10-4 M; 96 h) reduces HL-60 AML cell viability with high potency, corresponding to a pEC50 of 7.6 after 96 hours of incubation[2].
TH9028 (50 nM; 24 h) reduces DNA replication fork speed in HL-60 and THP-1 AML cells at a concentration of 50 nM after 24 hours of incubation[2].
TH9028 (10-10 to 10-4 M; 96 h) induced cell viability loss in HL-60 AML, THP-1 AML, and SW620 colorectal cancer cells, which was fully rescued by thymidine supplementation, confirming thymidine depletion as the mechanism of action[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60 AML cell line, THP-1 AML cell line, SW620 colorectal cancer cell line
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Concentration:0.1, 1, 10, 100 nM, 1, 10, 10 μM
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Incubation Time:96 h
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Result:Induced viability defects in HL-60, THP-1, and SW620 cells, which were completely rescued by thymidine supplementation.
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Animal Model:NOG mice[2]
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Dosage:30 mg/kg
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Administration:subcutaneous; twice daily
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Result:Extended median survival.
Reached peak plasma concentrations post-subcutaneous dosing.
Increased MTHFD2 protein thermal stability in tumor tissue (CETSA).
Caused no significant weight loss or hematological toxicity at therapeutic doses.
Chemical Information
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No. CAS 2379556-15-5
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Appearance Solid
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Peso molecular 458.39
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Fòrmula C16H18N12O5
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Color Light yellow to yellow
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SMILES
NC(NC(N)=NC1=O)=C1NC(NC2=CN=C(C(N[C@H](C(O)=O)CCC3=NN=NN3)=O)C=C2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
DMSO : 25 mg/mL (54.54 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; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (272 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jha V, et al. Selectivity analysis of diaminopyrimidine-based inhibitors of MTHFD1, MTHFD2 and MTHFD2L. Sci Rep. 2024;14(1):21073. Published 2024 Sep 10. [Content Brief]
[2]. Bonagas N, et al. Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress. Nat Cancer. 2022;3(2):156-172. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1815 mL | 10.9077 mL | 21.8155 mL | 54.5387 mL |
| 5 mM | 0.4363 mL | 2.1815 mL | 4.3631 mL | 10.9077 mL | |
| 10 mM | 0.2182 mL | 1.0908 mL | 2.1815 mL | 5.4539 mL | |
| 15 mM | 0.1454 mL | 0.7272 mL | 1.4544 mL | 3.6359 mL | |
| 20 mM | 0.1091 mL | 0.5454 mL | 1.0908 mL | 2.7269 mL | |
| 25 mM | 0.0873 mL | 0.4363 mL | 0.8726 mL | 2.1815 mL | |
| 30 mM | 0.0727 mL | 0.3636 mL | 0.7272 mL | 1.8180 mL | |
| 40 mM | 0.0545 mL | 0.2727 mL | 0.5454 mL | 1.3635 mL | |
| 50 mM | 0.0436 mL | 0.2182 mL | 0.4363 mL | 1.0908 mL |
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