CC214-1

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CC214-1 is a potentially efficacious mTOR inhibitor that induces autophagy ,with an IC₅₀ is 0.002 μM. CC214-1 proved to be useful as an in vitro tool compound for the exploration of mTOR kinase biology. CC214-1 can be used for Glioblastoma study.

For research use only. We do not sell to patients.

CC214-1 Chemical Structure

CAS No. : 1021920-32-0

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mTOR mTORC1 mTORC2

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Description

CC214-1 is a potentially efficacious mTOR inhibitor that induces autophagy ^[1],with an IC₅₀ is 0.002 μM. CC214-1 proved to be useful as an in vitro tool compound for the exploration of mTOR kinase biology. CC214-1 can be used for Glioblastoma study^[2].

IC₅₀ & Target ^[2]

mTOR

0.002 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	IC₅₀	0.018 μM Compound: 9a, CC214-1	Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKTS473 phosphorylation after 1 hr by sandwich immunoassay Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKTS473 phosphorylation after 1 hr by sandwich immunoassay	[PMID: 23414803]
PC-3	IC₅₀	0.04 μM Compound: 9a, CC214-1	Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr by sandwich immunoassay Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr by sandwich immunoassay	[PMID: 23414803]
PC-3	IC₅₀	0.224 μM Compound: 9a, CC214-1	Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST1 assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST1 assay	[PMID: 23414803]

In Vitro

CC214-1 (0, 0.1, 1, 2, 5, 10 μM, 8 h; 2 μM, 24 h) synergize with rapamycin (HY-10219), inhibiting mTORC1 signaling and tumor cell proliferation^[1].
CC214-1 (2 μM, 24 h) -mediated sensitivity to growth arrest in glioblastoma cells due to EGFRvIII expression and loss of PTEN^[1].
CC214-1 (5 μM, 0-48 h) massively lipidates LC3B-I to LC3B-II subtype and induces autophagy in GBM39 cells^[1].
CC214-1 has an IC₅₀ of mTOR is 0.002 μM^[2].
CC214-1 (0-10 μM, 4days) is efficient in inhibiting T cell activation and the expression of T-cell activation markers^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	glioblastoma
Concentration:	0, 0.1, 1, 2, 5, 10 μM; 2 μM
Incubation Time:	8 h; 24 h
Result:	Inhibited mTORC1 signaling in all glioblastoma cell lines tested, potently suppressing rapamycin-resistant 4E-BP1 and mTORC2 signaling. Inhibited mTORC1-dependent 4E-BP1 and S6 phosphorylation in EGFRvIII-expressing glioblastoma cells, as well as blocked glioblastoma cells overexpressing wild-type EGFR.

Immunofluorescence^[1]

Cell Line:	glioblastoma
Concentration:	2 μM, 5 μM
Incubation Time:	4 h; 0, 4, 12, 24, 48 h
Result:	Induced a transient expression of LC3B-II isoform and the conjugation of Atg12 to Atg5 indicative of the stimulation of the autophagy flux in U87EGFRvIII cell line. Massively lipidated LC3B-I to LC3B-II subtype and induces autophagy in GBM39 cells.

Cell Cycle Analysis^[3]

Cell Line:	glioblastoma
Concentration:	0-10 μM
Incubation Time:	4 day
Result:	Induced TEE cells in CD4+ and CD8+ T cell subsets.

Molecular Weight

391.43

Formula

C₂₀H₂₁N₇O₂

CAS No.

1021920-32-0

SMILES

O=C1NC2=NC=C(C3=CC=C(C4=NN=CN4)C=C3)N=C2N1CCC5CCOCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Gini B, et al. The mTOR kinase inhibitors, CC214-1 and CC214-2, preferentially block the growth of EGFRvIII-activated glioblastomas. Clin Cancer Res. 2013 Oct 15;19(20):5722-32. [Content Brief]

[2]. Mortensen DS, et al. Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1588-91. [Content Brief]

[3]. Herrero-Sánchez MC, et al. Effect of mTORC1/mTORC2 inhibition on T cell function: potential role in graft-versus-host disease control. Br J Haematol. 2016 Jun;173(5):754-68. [Content Brief]

CC214-1 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CC214-11021920-32-0mTORMammalian target of RapamycinGlioblastomacardiovascularautophagyInhibitorinhibitorinhibit

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