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MedKoo Cat#: 462324 | Name: SCH529074
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD. It can be used for the study of non-small-cell lung carcinoma (NSCLC).

Chemical Structure

SCH529074
SCH529074
CAS#922150-11-6

Theoretical Analysis

MedKoo Cat#: 462324

Name: SCH529074

CAS#: 922150-11-6

Chemical Formula: C31H36Cl2N6

Exact Mass: 562.2379

Molecular Weight: 563.57

Elemental Analysis: C, 66.07; H, 6.44; Cl, 12.58; N, 14.91

Price and Availability

Size Price Availability Quantity
5mg USD 570.00 2 Weeks
10mg USD 880.00 2 Weeks
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Related CAS #
No Data
Synonym
SCH529074; SCH-529074; SCH 529074
IUPAC/Chemical Name
N1-(2-((4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)quinazolin-4-yl)-N3,N3-dimethylpropane-1,3-diamine
InChi Key
NCAJLQDPTZBGJV-UHFFFAOYSA-N
InChi Code
InChI=1S/C31H36Cl2N6/c1-37(2)17-5-16-34-31-27-6-3-4-7-28(27)35-29(36-31)22-38-18-20-39(21-19-38)30(23-8-12-25(32)13-9-23)24-10-14-26(33)15-11-24/h3-4,6-15,30H,5,16-22H2,1-2H3,(H,34,35,36)
SMILES Code
CN(C)CCCNC1=C2C=CC=CC2=NC(CN3CCN(C(C4=CC=C(Cl)C=C4)C5=CC=C(Cl)C=C5)CC3)=N1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SCH529074 restores DNA binding activity and increases DNA binding affinity of R273H and R249S with Kd values of 0.6740 and 0.4313, respectively. SCH529074 also stimulates DNA binding activity and prevents human double minute-2 (Hdm-2) ubiquitination of wild-type p53 in vitro. SCH529074 reduces proliferation of tumor cell lines with mutant and wild-type p53 (EC50s = 400-3,700 nM), with the p53 mutant cell lines being the most sensitive.
In vitro activity:
Through its interaction with p53 DBD, SCH529074 restores DNA binding activity to mutant p53 and inhibits HDM2-mediated ubiquitination. SCH529074, that binds specifically to the p53 DBD in a saturable manner with an affinity of 1-2 microm. Reference: J Biol Chem. 2010 Apr 2;285(14):10198-212. https://pubmed.ncbi.nlm.nih.gov/20124408/
In vivo activity:
To be determined
Solvent mg/mL mM
Solubility
DMSO 20.0 35.49
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 563.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Nenkov M, Ma Y, Haase D, Zhou Z, Li Y, Petersen I, Lu G, Chen Y. Growth inhibitory role of the p53 activator SCH 529074 in non‑small cell lung cancer cells expressing mutant p53. Oncol Rep. 2020 Jun;43(6):2073-2082. doi: 10.3892/or.2020.7546. Epub 2020 Mar 17. PMID: 32186773. 2. Demma M, Maxwell E, Ramos R, Liang L, Li C, Hesk D, Rossman R, Mallams A, Doll R, Liu M, Seidel-Dugan C, Bishop WR, Dasmahapatra B. SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53. J Biol Chem. 2010 Apr 2;285(14):10198-212. doi: 10.1074/jbc.M109.083469. Epub 2010 Feb 2. PMID: 20124408; PMCID: PMC2856225.
In vitro protocol:
1. Nenkov M, Ma Y, Haase D, Zhou Z, Li Y, Petersen I, Lu G, Chen Y. Growth inhibitory role of the p53 activator SCH 529074 in non‑small cell lung cancer cells expressing mutant p53. Oncol Rep. 2020 Jun;43(6):2073-2082. doi: 10.3892/or.2020.7546. Epub 2020 Mar 17. PMID: 32186773. 2. Demma M, Maxwell E, Ramos R, Liang L, Li C, Hesk D, Rossman R, Mallams A, Doll R, Liu M, Seidel-Dugan C, Bishop WR, Dasmahapatra B. SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53. J Biol Chem. 2010 Apr 2;285(14):10198-212. doi: 10.1074/jbc.M109.083469. Epub 2010 Feb 2. PMID: 20124408; PMCID: PMC2856225.
In vivo protocol:
To be determined
1: Nenkov M, Ma Y, Haase D, et al. Growth inhibitory role of the p53 activator SCH 529074 in non‑small cell lung cancer cells expressing mutant p53. Oncol Rep. 2020;43(6):2073-2082. doi:10.3892/or.2020.7546 2: Nenkov M, Ma Y, Haase D, et al. Growth inhibitory role of the p53 activator SCH 529074 in non‑small cell lung cancer cells expressing mutant p53. Oncol Rep. 2020;43(6):2073-2082. doi:10.3892/or.2020.7546

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