2. PI3K/Akt/mTOR Autophagy
  3. mTOR Autophagy
  4. CC214-2

CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo.

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CC214-2

CC214-2 Chemical Structure

CAS No. : 1228012-18-7

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Based on 1 publication(s) in Google Scholar

CC214-2 Related Antibodies

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Description

CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo[1][2].

IC50 & Target[1][2]

mTORC1

 

mTORC2

 

Cellular Effect
Cell Line Type Value Description References
PC-3 IC50
0.315 μM
Compound: 10b, CC214-2
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
0.32 μM
Compound: 26, CC214-2
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr
[PMID: 26083478]
PC-3 IC50
0.386 μM
Compound: 10b, CC214-2
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
0.39 μM
Compound: 26, CC214-2
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr
[PMID: 26083478]
PC-3 IC50
1.55 μM
Compound: 10b, CC214-2
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 Vivo

CC214-2 (25 mg/kg, 50 mg/kg; po; once daily for 21 days) results tumor volume reductions in PC3 tumor xenograft model[1].
CC214-2 (30 mg/kg, 100 mg/kg; po; single dose) inhibits both mTORC1 (pS6) and mTORC2 (pAktS473) in vivo for at least 8 and 24 h, respectively[1].
CC214-2 (30 mg/kg; po) reduces M. tuberculosis CFU numbers and prevents mortality in mice with Chronic M. tuberculosis infection[1].
CC214-2 (50 mg/kg; po; once daily for 6 days) significantly reduces the growth of mouse U87EGFRvIII flank xenografts[2].
CC214-2 (100 mg/kg; po; once every 2 days for 6 days) inhibits mTORC1 and mTORC2 signaling in an intracranial glioblastoma model[2].

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

Animal Model: U87EGFRvIII flank xenografts in mice[2]
Dosage: 50 mg/kg
Administration: PO; once daily for 6 days
Result: Inhibited tumor growth.
Similarly activated autophagy in U87EGFRvIII xenografts.
Molecular Weight

383.44

Formula

C20H25N5O3
CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

O=C1N=C2NC=C(C3=CC=C(C(C)(C)O)N=C3)N=C2N(CC4CCOCC4)C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (163.00 mM; ultrasonic and warming and heat to 70°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6080 mL 13.0399 mL 26.0797 mL
5 mM 0.5216 mL 2.6080 mL 5.2159 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.41%

SDS (393 KB)

COA (248 KB) HNMR (259 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6080 mL 13.0398 mL 26.0797 mL 65.1992 mL
5 mM 0.5216 mL 2.6080 mL 5.2159 mL 13.0398 mL
10 mM 0.2608 mL 1.3040 mL 2.6080 mL 6.5199 mL
15 mM 0.1739 mL 0.8693 mL 1.7386 mL 4.3466 mL
20 mM 0.1304 mL 0.6520 mL 1.3040 mL 3.2600 mL
25 mM 0.1043 mL 0.5216 mL 1.0432 mL 2.6080 mL
30 mM 0.0869 mL 0.4347 mL 0.8693 mL 2.1733 mL
40 mM 0.0652 mL 0.3260 mL 0.6520 mL 1.6300 mL
50 mM 0.0522 mL 0.2608 mL 0.5216 mL 1.3040 mL
60 mM 0.0435 mL 0.2173 mL 0.4347 mL 1.0867 mL
80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8150 mL
100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6520 mL
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CC214-2 Related Classifications

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:

CC214-21228012-18-7mTORAutophagyMammalian target of RapamycinmTORC1mTORC2Mycobacterium tuberculosisautophagyTBInhibitorinhibitorinhibit

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