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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.81%
- CAS 番号: 2093449-12-6
- 分子式: C33H34Cl2FNO6
- 分子量:630.53
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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 |
化学情報
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CAS 番号 2093449-12-6
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性状 Solid
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分子量 630.53
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (282 KB)
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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-176083 関連分類
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