ASTX295
Based on 1 Customer Validation
ASTX295 is an orally active and selective MDM2 antagonist with an IC50 of <1 nM. ASTX295 inhibits the MDM2-p53 interaction, activates wild-type TP53, and thereby induces the expression of relevant transcriptional targets, leading to cell death. ASTX295 drives the transition of pancreatic cancer cells from senescence to apoptosis and regulates p53 and DNA damage biomarkers. ASTX295 can be used for the research of hematologic malignancies and pancreatic cancer.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 2093449-12-6
- Formula: C33H34Cl2FNO6
- Molecular Weight:630.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
ASTX295 (0-10000 nM; up to 72 h) reduces viability in all tested TP53WT lymphoid malignancy cell lines (DLBCL, MCL, T-cell lymphoma) with IC50 values of <1 nM to 100 nM over up to 72 h, induces p53 and p21 expression, and causes maximal cell death at 72 h (24 h in Z138 cells)[1].
ASTX295 (1 μM; 0-24 h, in combination with a p53 corrector) induces sustained upregulation of p53 signaling and DNA damage-related protein and mRNA biomarkers over a 24-hour period in BxPC3 (TP53: Y220C) cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC3 (TP53: Y220C)
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Concentration:1 μM (in combination with p53 corrector)
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Incubation Time:0, 2, 4, 6, 8, 24 h
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Result:Sustained upregulation of p53, phospho-p53 (S15), MDM2, p21, PUMA, phospho-CHK1 (S345), and phospho-H2A.X (S139) proteins through 24 h.
ASTX295 (80 mg/kg; p.o.; single dose) with PC14586 in BxPC3 tumor-bearing mice significantly increases the levels of p53 signaling pathway biomarkers (tissue p21, plasma GDF-15, p21/MDM2/GDF-15 mRNA in tumor tissue, and multiple protein biomarkers)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BxPC3-tumor bearing mice[2]
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Dosage:80 mg/kg
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Administration:p.o.; single dose; administered 3 hours after 100 mg/kg PC14586 p.o.
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Result:Increased relative tumor p21 levels up to ~45-fold relative to vehicle control at 16 hours post-dose.
Increased human GDF-15 levels in mouse plasma up to ~3.5 ng/ml at 16 hours post-dose, relative to PC14586 alone.
Upregulated tumor p21, MDM2, and GDF-15 mRNA at 16 hours post-dose.
Sustained upregulation of p53 signalling biomarkers (including p-p53 [S15], p21, PUMA, and p-H2A.X [S139]) at 16 hours post-dose by Western blotting.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2093449-12-6
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Appearance Solid
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Molecular Weight 630.53
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Formula C33H34Cl2FNO6
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Color White to off-white
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SMILES
CO[C@](C(C(C1=O)=C2)=C(F)C=C2[C@@](CC)(O)C3CCOCC3)(N1[C@H](C4=CC=C(Cl)C=C4)[C@H](C)C(O)=O)C5=CC=C(Cl)C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 41.18 mg/mL (65.31 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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)
Purity & Documentation
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Data Sheet (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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; -20°C, 1 month. 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 | 1.5860 mL | 7.9298 mL | 15.8597 mL | 39.6492 mL |
| 5 mM | 0.3172 mL | 1.5860 mL | 3.1719 mL | 7.9298 mL | |
| 10 mM | 0.1586 mL | 0.7930 mL | 1.5860 mL | 3.9649 mL | |
| 15 mM | 0.1057 mL | 0.5287 mL | 1.0573 mL | 2.6433 mL | |
| 20 mM | 0.0793 mL | 0.3965 mL | 0.7930 mL | 1.9825 mL | |
| 25 mM | 0.0634 mL | 0.3172 mL | 0.6344 mL | 1.5860 mL | |
| 30 mM | 0.0529 mL | 0.2643 mL | 0.5287 mL | 1.3216 mL | |
| 40 mM | 0.0396 mL | 0.1982 mL | 0.3965 mL | 0.9912 mL | |
| 50 mM | 0.0317 mL | 0.1586 mL | 0.3172 mL | 0.7930 mL | |
| 60 mM | 0.0264 mL | 0.1322 mL | 0.2643 mL | 0.6608 mL |
ASTX295 Related Classifications
HY-176083 Related Classifications
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