CC-223
Description References- Product Name
- CC-223
- CAS No.
- 1228013-30-6
- Chemical Name
- CC-223
- Synonyms
- CC-223;CS-2039;CS-2163;ATG-008;Onatasertib;CC223;CC 223;Onatasertib (CC-223);Onatasertib(CC 223,ATG-008);mTOR,ATG008,Mammalian target of Rapamycin,inhibit,ATG-008,Onatasertib,Inhibitor,ATG 008,Apoptosis;7-[6-(2-Hydroxypropan-2-yl)pyridin-3-yl]-1-(trans-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one
- CBNumber
- CB33041393
- Molecular Formula
- C21H27N5O3
- Formula Weight
- 397.47
- MOL File
- 1228013-30-6.mol
CC-223 Property
- Boiling point:
- 562.9±60.0 °C(Predicted)
- Density
- 1.37±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; ≥108 mg/mL in DMSO; ≥20.28 mg/mL in EtOH
- form
- crystalline solid
- pka
- 13?+-.0.29(Predicted)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 19917
- Product name
- CC-223
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $49
- Updated
- 2024/03/01
- Product number
- 19917
- Product name
- CC-223
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $179
- Updated
- 2024/03/01
- Product number
- 19917
- Product name
- CC-223
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $310
- Updated
- 2024/03/01
- Product number
- 19917
- Product name
- CC-223
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $534
- Updated
- 2024/03/01
- Product number
- CS-4560
- Product name
- CC-223
- Purity
- 99.43%
- Packaging
- 50mg
- Price
- $900
- Updated
- 2021/12/16
CC-223 Chemical Properties,Usage,Production
Description
CC-223 is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, demonstrating inhibition of mTORC1 (pS6RP and p4EBP1) and mTORC2 [pAKT(S473)] in cellular systems. After tumor-bearing mice was treated with CC-223 for a single oral dose. It exhibited dose-dependent tumor growth inhibition in multiple solid tumor xenografts. The observed antitumor activity of CC-223 is likely to be mediated through inhibition of both mTORC1 and mTORC2. CC-223 is currently in phase I clinical trials for its treatment of advanced solid and hematologic cancers.
References
Varga, Andrea, et al. "Phase I expansion trial of an oral TORC1/TORC2 inhibitor (CC-223) in advanced solid tumors." Journal of Clinical Oncology 31.15(2013):-.
Mortensen, D. S., et al. "CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization." Molecular Cancer Therapeutics 14.6(2015):1295.
Goy, A, et al. "Phase I expansion trial of an oral TORC1/TORC2 inhibitor (CC-223) in diffuse large B-cell lymphoma (DLBCL) and multiple myeloma (MM)." Neuroendocrinology 43.3(2013):276-276.
Shih, Kent C, et al. "Phase I trial of an oral TORC1/TORC2 inhibitor (CC-223) in advanced solid and hematologic cancers." Journal of Clinical Oncology (2012).
Description
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
References
[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.
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View Lastest Price from CC-223 manufacturers
- Product
- 7-[6-(2-Hydroxy-2-propanyl)-3-pyridinyl]-1-(trans-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one 1228013-30-6
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2019-12-23