ChemicalBook CAS DataBase List 1228012-18-7

1228012-18-7

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]-
CAS	1228012-18-7
Molecular Formula	C20H25N5O3
Molecular Weight	383.44
MOL File	1228012-18-7.mol

Chemical 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

Hazard Information

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

storage

Store at -20°C

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

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