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SCH 529074

Product Name
SCH 529074
CAS No.
922150-11-6
Chemical Name
SCH 529074
Synonyms
SCH 529074;SCH529074, 10 mM in DMSO;N3-[2-[[4-[Bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-1,3-propanediamine;N1-(2-((4-(Bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)quinazolin-4-yl)-N3,N3-dimethylpropane-1,3-diamine;1,3-Propanediamine, N3-[2-[[4-[bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-
CBNumber
CB93146379
Molecular Formula
C31H36Cl2N6
Formula Weight
563.56
MOL File
922150-11-6.mol
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SCH 529074 Property

Boiling point:
640.3±55.0 °C(Predicted)
Density 
1.262±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 33 mg/ml; DMSO: 25 mg/ml; Ethanol: 33 mg/ml
form 
A crystalline solid
pka
9.44±0.28(Predicted)
color 
Off-white to light yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21552
Product name
SCH 529074
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
21552
Product name
SCH 529074
Purity
≥98%
Packaging
5mg
Price
$139
Updated
2024/03/01
Cayman Chemical
Product number
21552
Product name
SCH 529074
Purity
≥98%
Packaging
10mg
Price
$230
Updated
2024/03/01
Cayman Chemical
Product number
21552
Product name
SCH 529074
Purity
≥98%
Packaging
25mg
Price
$533
Updated
2024/03/01
Tocris
Product number
4240
Product name
SCH529074
Purity
≥98%(HPLC)
Packaging
50
Price
$710
Updated
2021/12/16
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SCH 529074 Chemical Properties,Usage,Production

Description

SCH 529074 is a small molecule activator of p53, a tumor suppressor that is mutated or non-functional in 50% of human tumors. SCH 529074 restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 DNA binding domains (R273H and R249S) in an electrophoretic mobility shift assay with Kd values of 0.6740 and 0.4313, respectively. It also stimulates DNA binding activity and prevents human double minute-2 (Hdm-2) ubiquitination of wild-type p53 in vitro. SCH 29074 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 vivo, SCH 529074 reduces tumor growth in a DLD-1 human colorectal cancer xenograft model in mice in a dose-dependent manner.

Uses

SCH 529074 is 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 ubiquination of wild type p53.

in vivo

SCH529074 (oral administration; 30 or 50 mg/kg; twice daily; 4 weeks; started on day 3 until day 31) causes 79 and 43% reduction of tumor growth at 50 and 30 mg/kg doses, respectively. the degree of tumor inhibition correlates with the plasma exposure of the compound (0.26–0.55 μm?at 30 mg/kg and 0.39-0.79 μm?at 50 mg/kg, 2-12 h post final dosing) in human DLD-1 colorectal cancer xenograft[2].

Animal Model:Female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells[2]
Dosage:30 or 50 mg/kg
Administration:Oral administration; twice daily; 4 weeks; started on day 3 until day 31
Result:Inhibited tumor growth

References

[1] MARK DEMMA. 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]. The Journal of Biological Chemistry, 2010: 10198-10212. DOI: 10.1074/jbc.m109.083469

SCH 529074 Preparation Products And Raw materials

Raw materials

Preparation Products

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SCH 529074 Suppliers

China 46 United Kingdom 1 United States 4 Global 51
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
Shanghai Yu Ben Biotechnology Co., Ltd.
Tel
021-61350663 15502154572
Fax
-
Email
1639466865@qq.com
Country
China
ProdList
498
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
Advantage
58
Career Henan Chemica Co
Tel
+86-0371-86658258 +8613203830695
Fax
0371-86658258
Email
laboratory@coreychem.com
Country
China
ProdList
30229
Advantage
58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
ProdList
11218
Advantage
58
Guangzhou Younan Technology Co., Ltd
Tel
020-82000279 18988941452
Fax
QQ：3283937693
Email
YN_research@163.com
Country
China
ProdList
3011
Advantage
58
ShangHai ChuanQian Chemcial Technique Centre
Tel
15869524721
Email
3525679403@qq.com
Country
China
ProdList
4989
Advantage
58
MedBioPharmaceutical Technology Inc
Tel
021-69568360 18916172912
Email
order@med-bio.cn
Country
China
ProdList
8140
Advantage
58

922150-11-6, SCH 529074Related Search:


  • N3-[2-[[4-[Bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-1,3-propanediamine
  • SCH 529074
  • 1,3-Propanediamine, N3-[2-[[4-[bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-
  • N1-(2-((4-(Bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)quinazolin-4-yl)-N3,N3-dimethylpropane-1,3-diamine
  • SCH529074, 10 mM in DMSO
  • 922150-11-6