CC-223 Struktur

CC-223

Bezeichnung:CC-223

CAS-Nr1228013-30-6

Englisch Name:CC-223

CBNumberCB33041393

SummenformelC21H27N5O3

Molgewicht397.47

MOL-Datei1228013-30-6.mol

CC-223 physikalisch-chemischer Eigenschaften

Siedepunkt	562.9±60.0 °C(Predicted)
Dichte	1.37±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	insoluble in H2O; ≥108 mg/mL in DMSO; ≥20.28 mg/mL in EtOH
Aggregatzustand	crystalline solid
pka	13?+-.0.29(Predicted)
Farbe	Light yellow to yellow

Gefahreninformationscode (GHS)

CC-223 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
CC-223 is a potent inhibitor of mTOR (IC₅₀ = 16 nM) that shows selectivity for mTOR over a panel of 246 other kinases. It blocks signaling through both mTORC1 and mTORC2, inhibiting the phosphorylation of S6RP, 4EBP1, and Akt(S473) in cellular systems. CC-223 inhibits growth and induces apoptosis in hematologic and solid tumor cell lines in vitro, and it exhibits dose-dependent tumor growth inhibition in multiple solid tumor xenografts in vivo.
in vitro
cc-223 was identified as an atp–competitive inhibitor of the mtor kinase targeting mtorc1 of both 4ebp1 and p70 s6 kinase 1 and mtorc2, which prevented the upregulation of akt phosphorylation. moreover, cc-223 was selectively potent to mtor kinase while showed more than 150-fold sensitivity against the related lipid kinase, pi3ka. in addition, cc-223 was active over many non-hodgkin lymphoma cell lines and solid tumor lines such as including glioma, breast, hepatocellular carcinoma, as well as non–small cell lung cancer [1].
in vivo
in animal study, cc-223 was selected for evaluation in pc-3 tumor bearing efficacy mouse models. mice were orally treated with vehicle or various doses of cc-223 once daily or twice daily at a dose of 5 ml/kg for 21 days, and the final reductions of tumor volume were measured following the final day of dosing. results showed that all cc-223 had dose- and schedule-dependent inhibition of tumor growth in the pc-3 model. moreover, the maximum observed efficacy for cc-223 was determined to be 87%, at its tolerated dose of 25 mg/kg q.d. [1].
IC 50
16 nm
Einzelnachweise
[1] mortensen ds, et al. discovery of mammalian target of rapamycin (mtor) kinase inhibitor cc-223. j med chem. 2015 jul 9;58(13):5323-5333.
[2] bendell jc, et al. a phase i dose-escalation study to assess safety, tolerability, pharmacokinetics, and preliminary efficacy of the dual mtorc1/mtorc2 kinase inhibitor cc-223 in patients with advanced solid tumors or multiple myeloma. cancer. 2015 oct 1;121(19):3481-90.

CC-223 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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