MD-224 |
| カタログ番号GC38812 |
MD-224 は、タンパク質分解標的キメラ (PROTAC) の概念に基づいた、ファースト イン クラスで非常に強力な低分子ヒト マウス ダブル ミニッツ 2 (MDM2) 分解剤です。 MD-224 は、Cereblon と MDM2 のリガンドで構成されています。 MD-224 は、ヒト白血病細胞において <1 nM の濃度で MDM2 の急速な分解を誘導し、RS4;11 細胞の増殖の阻害において 1.5 nM の IC50 値を達成します。 MD-224 は、新しいクラスの抗がん剤になる可能性があります。
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Cas No.: 2136247-12-4
Sample solution is provided at 25 µL, 10mM.
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MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent[1].
MD-224 (1-30 nM; 2 hours) effectively induces depletion of MDM2 protein and concurrently accumulation of p53 protein in a dose-dependent manner in RS4;11 cells[1].MD-224 (30 nM; 6 hours) is more potent than MI-1061 in induction of transcriptional upregulation of these p53 target genes but have no effect on TP53 itself in RS4;11 cells[1].MD-224 (0.001-1 μM; 24 hours) induces robust apoptosis at ≤10 nM in a dose-dependent manner upon a 24 hours treatment[1]. Western Blot Analysis[1] Cell Line: RS4;11 cells
[1]. Li Y, et al. Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis TargetingChimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable TumorRegression. J Med Chem. 2019 Jan 24;62(2):448-466
| Cas No. | 2136247-12-4 | SDF | |
| Canonical SMILES | FC1=C(Cl)C=CC=C1[C@@H]2[C@@]3(C(C=CC(Cl)=C4)=C4NC3=O)C5(CCCCC5)N[C@H]2C(NC6=CC=C(C(NCCCC#CC7=C(CN(C8C(NC(CC8)=O)=O)C9=O)C9=CC=C7)=O)C=C6)=O | ||
| Formula | C48H43Cl2FN6O6 | M.Wt | 889.8 |
| 溶解度 | DMSO: 150 mg/mL (168.58 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1238 mL | 5.6192 mL | 11.2385 mL |
| 5 mM | 0.2248 mL | 1.1238 mL | 2.2477 mL |
| 10 mM | 0.1124 mL | 0.5619 mL | 1.1238 mL |
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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