Home PI3K/Akt/mTOR mTOR inhibitor Onatasertib (CC 223) For research use only.

Onatasertib (CC 223)

Synonyms: ATG-008

Onatasertib (CC 223) is a potent, selective, and orally bioavailable mTOR inhibitor with IC50 of 16 nM, >200-fold selectivity over the related PI3K-α. Phase 1/2.

Onatasertib (CC 223) Chemical Structure

Onatasertib (CC 223) Chemical Structure

CAS: 1228013-30-6

Selleck's Onatasertib (CC 223) has been cited by 2 Publications

1 Customer Review

Purity & Quality Control

Batch: S788601 DMSO] 79 mg/mL] false] Ethanol] 79 mg/mL] false] Water] Insoluble] false Purity: 99.57%
99.57

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Signaling Pathway

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human PC3 cells Function assay 1 h Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr, IC50=0.01 μM 26083478
human PC3 cells Function assay 1 h Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr 26083478
human PC3 cells Function assay 1 h Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr 26083478
Click to View More Cell Line Experimental Data

Biological Activity

Description Onatasertib (CC 223) is a potent, selective, and orally bioavailable mTOR inhibitor with IC50 of 16 nM, >200-fold selectivity over the related PI3K-α. Phase 1/2.
Targets
mTOR [1]
(Cell-free assay)		 cFMS [1]
(Cell-free assay)		 FLT4 [1]
(Cell-free assay)		 DNA-PK [1]
(Cell-free assay)
16 nM 28 nM 651 nM 840 nM
In vitro
In vitro In a panel of cell lines, CC-223 inhibits both mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] markers with IC50 ranges of 27 to 184 nM for pS6RP, 120 to 1,050 nM for p4EBP1 and 11 to 150 nM for pAKT(S473), respectively. CC-223 also inhibits cell growth and induces apoptosis across a number of cancer cell lines. [1]
Kinase Assay Kinase assays mTOR.
Reagents are prepared as follows:”Simple Tor buffer”: 10mM Tris pH 7.4, 100mM NaCl, 0.1% Tween-20, 1mM DTT. Recombinant mTOR is diluted in this buffer to an assay concentration of 0.200ug/mL. ATP/Substrate solution: 0.075 mM ATP, 12.5 mM MnCl2, 50 mM Hepes, pH 7.4, 50mM β-GOP, 250 nM Microcystin LR, 0.25 mM EDTA, 5 mM DTT, and 3.5 μg/mL GST-p70S6. Dilution Curve: A 10-point, 1:3 dilution of compounds are prepared in neat DMSO at 50 times the final assay concentration. Detection reagent mix: 50 mM HEPES, pH 7.4 0.01% Triton X-100, 0.01% BSA, 0.1 mM EDTA, 12.7 ug/mL Cy5-anti-GST antibody, 9 ng/ml anti-phospho p70S6 antibody (Thr389), 627ng/mL anti-mouse IgG labeled with Lance Eu. To 20 uL of the Simple Tor buffer is added 0.5 uL of the compound Dilution Curve in DMSO. The final concentration range for compound is 30 to 0.0015 μM. To initiate the reaction, 5 μL of the ATP/substrate solution is added to the above. The reaction is allowed to run for 60 minutes. The assay is stopped by adding 5 μL of 60 mM EDTA. Ten (10) μL of detection reagent mix is then added, and the mixture is allowed to sit at least 2 hours before reading on a Perkin Elmer Envision microplate reader set to detect Europium-based TR-FRET.
Cell Research Cell lines PC-3, CAL-51, A549,T47D,NCI-H460, HepG2, AU565, Hep3B, HCC, U87MG, HCT116, MDA-MB-231, and NCI-H23 cells
Concentrations ~ 10 μM
Incubation Time 72 h
Method Compound is spotted via an acoustic dispenser (EDC ATS-100) into an empty 384-well plate. Cells are diluted to desired densities and added directly to the compound-spotted plates. Cells are allowed to grow for 72 hours. Viability is assessed via Cell Titer-Glo. All data are normalized and represented as a percentage of the DMSO-treated cells. Results are then expressed as GI50 and/or IC50 values.
In Vivo
In vivo In PC-3 tumor-bearing mice, CC-223 (25 mg/kg, p.o.) inhibits both mTORC1 and mTORC2. CC-223 (25 mg/kg, p.o.) also results in tumor growth inhibition by 47% to 95% in xenograft models of prostate, glioma, breast, lung, and colon. [1]
Animal Research Animal Models Mice bearing PC-3, U-87 MG, HCT 116, MDA-MB-231, or A549 tumors
Dosages 25 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02031419 Active not recruiting
Lymphoma Large B-Cell Diffuse
Celgene
 December 18 2013 Phase 1
NCT01545947 Completed
Carcinoma Non-Small-Cell Lung|Non-Small Cell Lung Cancer
Celgene
 May 1 2012 Phase 1
NCT01177397 Completed
Multiple Myeloma|Diffuse Large B-Cell Lymphoma|Glioblastoma Multiforme|Hepatocellular Carcinoma|Non-Small Cell Lung Cancer|Neuroendocrine Tumors of Non-Pancreatic Origin|Hormone Receptor-Positive Breast Cancer
Celgene
 July 20 2010 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 397.47 Formula

C21H27N5O3
CAS No. 1228013-30-6 SDF Download Onatasertib (CC 223) SDF
Smiles CC(C)(C1=NC=C(C=C1)C2=CN=C3C(=N2)N(C(=O)CN3)C4CCC(CC4)OC)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (198.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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