WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 202841
Description: TAS-109, also known as DFP-10917 and CNDAC, is an analogue of the nucleoside deoxycytidine with potential antineoplastic activity. Nucleoside analogue TAS-109 is incorporated into DNA and directly inhibits the activity of DNA polymerase, which may result in inhibition of DNA replication and cell cycle arrest in the S and G2/M phases, DNA fragmentation, and tumor cell apoptosis.
MedKoo Cat#: 202841
Chemical Formula: C10H12N4O4
Exact Mass: 252.08585
Molecular Weight: 252.22668
Elemental Analysis: C, 47.62; H, 4.80; N, 22.21; O, 25.37
Synonym: TAS109; TAS109; TAS 109; DFP-10917; DFP 10917; DFP10917; CNDAC; Radgocitabine
IUPAC/Chemical Name: (2R,3S,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-hydroxy-5-(hydroxymethyl)oxolane-3-carbonitrile
InChi Key: DCYBPMFXJCWXNB-JWIUVKOKSA-N
InChi Code: InChI=1S/C10H12N4O4/c11-3-5-8(16)6(4-15)18-9(5)14-2-1-7(12)13-10(14)17/h1-2,5-6,8-9,15-16H,4H2,(H2,12,13,17)/t5-,6+,8-,9+/m0/s1
SMILES Code: N#C[C@@H]1[C@H](N2C=CC(N)=NC2=O)O[C@H](CO)[C@H]1O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 252.22668 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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TAS-109 is a novel deoxycitidine analogue with unique mechanism of action. Brief exposure to high concentrations of TAS-109 inhibits DNA polymerase resulting in S-phase arrest, while prolonged exposure to TAS-109 at low concentration causes DNA fragmentation, G2/M phase arrest and apoptosis. TAS-109 demonstrated activity in tumor xenografts resistant to other deoxycitidine analogs. CI of TAS-109 is feasible and well tolerated with myelosuppression as main DLT. The recommended doses are 2 mg/mÂ²/day and 3 mg/mÂ²/day on the 14-day and 7-day CI schedules respectively. Preliminary activity was suggested. PD data demonstrate biological activity at the tested doses. see http://meeting.ascopubs.org/cgi/content/abstract/26/15_suppl/2577.