CEP-28122 Struktur

CEP-28122

Bezeichnung:CEP-28122

CAS-Nr1022958-60-6

Englisch Name:CEP-28122

CBNumberCB42666714

SummenformelC28H35ClN6O3

Molgewicht539.07

MOL-Datei1022958-60-6.mol

CEP-28122 physikalisch-chemischer Eigenschaften

Siedepunkt	786.9±70.0 °C(Predicted)
Dichte	1.357±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	≤30mg/ml in DMSO;12mg/ml in dimethyl formamide
Aggregatzustand	crystalline solid
pka	16.24±0.40(Predicted)

CEP-28122 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
CEP-28122 is used as an orally efficacious inhibitor of (ALK), analplastic lymphoma kinase, in the treatment of cancer.
Biologische Aktivität
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).
Einzelnachweise
[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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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