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SCH529074 is a selective activator of p53 (Ki = 1 μM) and can be used in studies about non-small-cell lung carcinoma. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 28 € | In Stock | |
2 mg | 36 € | In Stock | |
5 mg | 55 € | In Stock | |
10 mg | 100 € | In Stock | |
25 mg | 220 € | In Stock | |
50 mg | 327 € | In Stock | |
100 mg | 468 € | In Stock | |
1 mL x 10 mM (in DMSO) | 65 € | In Stock |
Description | SCH529074 is a selective activator of p53 (Ki = 1 μM) and can be used in studies about non-small-cell lung carcinoma. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. |
Targets&IC50 | p53 DBD:1-2 μM (Ki) |
In vitro | SCH529074 (2-4 µM) reduces cell viability and decreases to 20-25% in p53 mutant cells including H157, H1975, and H322, and to 68% in the p53 WT cell line A549 at 4 µM. SCH 529074 (2-4 µM) induces NSCLC cells including H157, A549, HCT116, and HCT116 p53-/- arrested at the G0/G1 phase (59%; 72%; 66%; and 57%)[2]. |
In vivo | In female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells, SCH529074 (orally; 30 and 50 mg/kg) reduces 79 and 43% of tumor growth with the plasma exposure of 0.26–0.55 μm at 30 mg/kg and 0.39-0.79 μm at 50 mg/kg[1]. |
Alias | SCH 529074 |
Molecular Weight | 563.56 |
Formula | C31H36Cl2N6 |
Cas No. | 922150-11-6 |
Smiles | CN(C)CCCNc1nc(CN2CCN(CC2)C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)nc2ccccc12 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | Ethanol: 33 mg/mL DMF: 33 mg/mL DMSO: 22.5 mg/mL (39.9 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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