4-Amino-1-[(2S)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]pyrimidin-2-one

Name	TROXACITABINE
Synonyms	CS-150 (-)-Occc (-)-Bch 204 TROXACITABINE Lamivudine Impurity I (Troxacitabine) 4-Amino-1-[(2S)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]pyrimidin-2-one 4-amino-1-[(2S,4S)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]-1,2-dihydropyrimidin-2-one TROXACITABINE,2(1H)-PYRIMIDINONE, 4-AMINO-1-(2-(HYDROXYMETHYL)-1,3-DIOXOLAN-4-YL)-, (2S-CIS)-
CAS	145918-75-8
EINECS	200-258-5

Molecular Formula	C8H11N3O4
Molar Mass	213.19
Density	1.71±0.1 g/cm3(Predicted)
Melting Point	176-177°
Boling Point	422.5±55.0 °C(Predicted)
Specific Rotation(α)	D25 -38.33° (c = 0.43 in MeOH).
Solubility	DMSO (Slightly), Methanol (Slightly)
Appearance	Solid
Color	White to Off-White
pKa	14.83±0.10(Predicted)
Storage Condition	2-8°C(protect from light)
Stability	Hygroscopic
In vitro study	Troxacitabine has shown cutotoxicity in cancer cell lines of hepatocellular (HepG2), prostate (PC3, DUI45), non-small cell lung (NCI-H460, NCr-322M) colon (HT29), renal (CAK-l, A498, RXF-393, SNI2-C) and pancreatic origin (Pnac-Ol, MiaPa Ca) with IC 50 s range from 15-35 μM.
In vivo study	Troxacitabine is highly active against the Panc-01 model, with TGI levels of 88.5% and 84.3% at the 10 and 25 mg/kg doses, respectively. The mean final tumor weights for animals given troxacitabine are also significantly smaller compared with vehicle controls. Troxacitabine has less activity against the MiaPaCa model. Troxacitabine is very effective in human RCC tumor xenograft models, including CAM-i, A498, RXF-393, and SN12C carcinomas. Very good responses are ob served in animals bearing CAM-i, A498, and RXF-393 RCC tumors given i.p. doses of 10, 25, and 50 mg/kg twice a day for 5 days.

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