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
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)
N-Bromosuccinimide Price
- Product number
- 18406
- Product name
- CEP-28122
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 18406
- Product name
- CEP-28122
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $193
- Updated
- 2024/03/01
- Product number
- 18406
- Product name
- CEP-28122
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $341
- Updated
- 2024/03/01
- Product number
- 18406
- Product name
- CEP-28122
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $745
- Updated
- 2024/03/01
- Product number
- C256650
- Product name
- CEP-28122
- Packaging
- 25mg
- Price
- $10725
- Updated
- 2021/12/16
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
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View Lastest Price from CEP-28122 manufacturers
- 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