Pyrazino[2,3-b]pyrazin-2(1H)-one, 3,4-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-4-[(tetrahydro-2H-pyran-4-yl)methyl]-
![Pyrazino[2,3-b]pyrazin-2(1H)-one, 3,4-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-4-[(tetrahydro-2H-pyran-4-yl)methyl]- Structure](CAS/20210305/GIF/1228012-18-7.gif)
- CAS No.
- 1228012-18-7
- Chemical Name:
- Pyrazino[2,3-b]pyrazin-2(1H)-one, 3,4-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-4-[(tetrahydro-2H-pyran-4-yl)methyl]-
- Synonyms
- CC214-2;6-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-4-((tetrahydro-2H-pyran-4-yl)methyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one;Pyrazino[2,3-b]pyrazin-2(1H)-one, 3,4-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-4-[(tetrahydro-2H-pyran-4-yl)methyl]-
- CBNumber:
- CB110785202
- Molecular Formula:
- C20H25N5O3
- Molecular Weight:
- 383.44
- MDL Number:
- MOL File:
- 1228012-18-7.mol
Pyrazino[2,3-b]pyrazin-2(1H)-one, 3,4-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-4-[(tetrahydro-2H-pyran-4-yl)methyl]- Properties
| Boiling point | 569.8±60.0 °C(Predicted) |
|---|---|
| Density | 1.39±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMSO : 12.5 mg/mL (32.60 mM; ultrasonic and warming and heat to 80°C) |
| form | Solid |
| pka | 13.67±0.29(Predicted) |
| color | Light yellow to light brown |
Pyrazino[2,3-b]pyrazin-2(1H)-one, 3,4-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-4-[(tetrahydro-2H-pyran-4-yl)methyl]- Chemical Properties,Uses,Production
Uses
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].
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. tuberculosisinfection[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].
| 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. |
IC 50
mTORC1; mTORC2
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. DOI:10.1158/1078-0432.CCR-13-0527
[2] Tasneen R, et al. Dual mTORC1/mTORC2 Inhibition as a Host-Directed Therapeutic Target in Pathologically Distinct Mouse Models of Tuberculosis. Antimicrob Agents Chemother. 2021;65(7):e0025321. DOI:10.1128/AAC.00253-21
Pyrazino[2,3-b]pyrazin-2(1H)-one, 3,4-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-4-[(tetrahydro-2H-pyran-4-yl)methyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
Pyrazino[2,3-b]pyrazin-2(1H)-one, 3,4-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-4-[(tetrahydro-2H-pyran-4-yl)methyl]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Aladdin Scientific | tp@aladdinsci.com | United States | 52923 | 58 | |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3506 | 58 |
| Lanzhou Kangyuxin Biotechnology Co., Ltd. | 0931-4190454 13893344397 | sales@kyxpharma.com | China | 3151 | 58 |
| ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 4989 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29257 | 58 |
| Jiangsu Aikon Biopharmaceutical R&D Co.,Ltd | 025-58851090 17714375163 | 2881759498@qq.com | China | 13011 | 58 |
