ChemicalBook > CAS DataBase List > CEP-28122

CEP-28122

Product Name
CEP-28122
CAS No.
1022958-60-6
Chemical Name
CEP-28122
Synonyms
CS-1605;CEP-28122;CEP 28122;CEP28122;(1S,2S,3R,4R)-3-[[5-Chloro-2-[[(7S)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-bicyclo[2.2.1]hept-5-ene-2-carboxamide;Bicyclo[2.2.1]hept-5-ene-2-carboxamide, 3-[[5-chloro-2-[[(7S)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-, (1S,2S,3R,4R)-;(1S,2S,3R,4R)-3-[5-chloro-2-((S)-1-methoxy-7-morpholin-4-yl-6,7,8,9-tetrahydro-5H-benzo[a]cyclohepten-2-ylamino)pyrimidin-4-ylamino]bicyclo[2.2.1]hept-5-ene-2-carboxylic acid amide
CBNumber
CB42666714
Molecular Formula
C28H35ClN6O3
Formula Weight
539.07
MOL File
1022958-60-6.mol
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CEP-28122 Property

Boiling point:
786.9±70.0 °C(Predicted)
Density 
1.357±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≤30mg/ml in DMSO;12mg/ml in dimethyl formamide
form 
crystalline solid
pka
16.24±0.40(Predicted)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
18406
Product name
CEP-28122
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
18406
Product name
CEP-28122
Purity
≥98%
Packaging
5mg
Price
$193
Updated
2024/03/01
Cayman Chemical
Product number
18406
Product name
CEP-28122
Purity
≥98%
Packaging
10mg
Price
$341
Updated
2024/03/01
Cayman Chemical
Product number
18406
Product name
CEP-28122
Purity
≥98%
Packaging
25mg
Price
$745
Updated
2024/03/01
TRC
Product number
C256650
Product name
CEP-28122
Packaging
25mg
Price
$10725
Updated
2021/12/16
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CEP-28122 Chemical Properties,Usage,Production

Uses

CEP-28122 is used as an orally efficacious inhibitor of (ALK), analplastic lymphoma kinase, in the treatment of cancer.

Biological Activity

cep-28122, a highly potent, selective, orally bioavailable inhibitor of alk, dampens the phosphorylation of alk and alk substrates in cells and triggers cytotoxicity or growth inhibition of alk-positive cancer cells with a favorable pharmaceutical and pharmacokinetic profile and selective pharmacologic efficacy. cep-28122 blocks alk tyrosine phosphorylation in tumor xenografts in mice. alk, which is constitutively activated in many human cancer types because of point mutations, gene amplification, and chromosomal translocations, has emerged as an excellent molecular target for cancer therapy.

in vitro

cep-28122, concentration-dependently, triggered growth inhibition/cytotoxicity of alk-positive anaplastic large-cell lymphoma (alcl) via inhibiting nucleophosmin (npm) -alk tyrosine (664) phosphorylation. due to the cep-28122 treatment, eml4-alk tyrosine phosphorylation was blocked in non-small cell lung cancer (nsclc) nci-h2228 and nci-h3122 cells and full-length alk receptor tyrosine phosphorylation was inhibited in neuroblastoma cell line nb-1 cells [1].

in vivo

severe combined immunodeficient (scid) mice bearing sup-m2 (b) or nu/nu mice bearing colon carcinoma hct-116 (c) subcutaneous tumor xenografts were administered orally with cep-28122 at 3, 10, or 30 mg/kg for 24 days. cep-28122 showed inhibition of alk tyrosine phosphorylation in a dose-dependent manner in tumor xenografts in mice when treated at 30 mg/kg. moreover, cep-28122 displayed dose-dependent antitumor activity in alk-positive alcl, nsclc, and neuroblastoma tumor xenografts in mice when administered orally at 30 mg/kg or higher [1].

IC 50

1.9 nm: blocks anaplastic lymphoma kinase (alk).

References

[1]. cheng, m., quail, m., gingrich, d., ott, g., lu, l., & wan, w. et al. cep-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers. molecular cancer therapeutics. 2011; 11(3): 670-679.

CEP-28122 Preparation Products And Raw materials

Raw materials

Preparation Products

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CEP-28122 Suppliers

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View Lastest Price from CEP-28122 manufacturers

Career Henan Chemical Co
Product
CEP-28122 1022958-60-6
Price
US $1.00/KG
Min. Order
1KG
Purity
95-99%
Supply Ability
1ton
Release date
2019-12-31

1022958-60-6, CEP-28122Related Search:


  • CS-1605
  • CEP 28122;CEP28122
  • CEP-28122
  • (1S,2S,3R,4R)-3-[[5-Chloro-2-[[(7S)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-bicyclo[2.2.1]hept-5-ene-2-carboxamide
  • (1S,2S,3R,4R)-3-[5-chloro-2-((S)-1-methoxy-7-morpholin-4-yl-6,7,8,9-tetrahydro-5H-benzo[a]cyclohepten-2-ylamino)pyrimidin-4-ylamino]bicyclo[2.2.1]hept-5-ene-2-carboxylic acid amide
  • Bicyclo[2.2.1]hept-5-ene-2-carboxamide, 3-[[5-chloro-2-[[(7S)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-, (1S,2S,3R,4R)-
  • 1022958-60-6
  • C28H35ClN6O3
  • Inhibitors
  • Amines, Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals