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5mg |
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10mg |
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Other Sizes |
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ln Vitro |
At 4, 24, and 72 hours of exposure, the cytidine ethinyl IC50 values in five human cancers were 0.114 to 1.032 μM, 0.015 to 0.067 μM, and 0.008 to 0.058 μM, respectively. These findings suggest that cytidine ethinyl's cytotoxicity tends to rise with longer exposure times. At the 24-hour exposure time, cytidine ethinyl seemed to demonstrate adequately strong cytotoxicity against all five human cancers, and the difference in IC50 values between the 24- and 72-hour exposure times was not significant. Cytidine ethinyl exhibits strong cytotoxicity even after four hours of treatment, as evidenced by IC50 values in four out of five human malignancies at submicromolar doses [1].
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ln Vivo |
Tumor growth inhibition ratio (IR) on day 15 of approximately OCUM-2MD3 and LX-1 xenografts showed tumor regression and a strong antitumor effect at the lowest toxic dose of cytidine ethinyl. 90% or higher. TAS-106 in each of the three management schemes. Specifically, once-weekly treatment with 6 mg/kg cytidine ethinyl resulted in a 98% internal rate of decay (IR) for LX-1 tumors. While once-weekly cytidine ethinyl treatment has an IR of less than 60% and a very weak anti-tumor effect, treatment with cytidine ethinyl three or five times a week has an effective anti-tumor effect with an IR of about 85%[1].
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References | |
Additional Infomation |
3'-C-Ethynylcytidine is a pyrimidine nucleoside.
TAS-106 is a new nucleoside antimetabolite. TAS-106 has demonstrated strong antitumor activity without serious toxicity in nude rat models bearing human tumours. 3'-C-ethynylcytidine is a synthetic cytidine nucleoside containing a covalently bound ethynyl group with potential antineoplastic and radiosensitizing activities. 3'-C-ethynylcytidine is metabolized in tumor cells to ethynylcytidine triphosphate (ECTP), which inhibits RNA synthesis by competitive inhibition of RNA polymerases I, II and III; subsequently, RNase L is activated, resulting in apoptosis. RNase L is a potent antiviral and antiproliferative endoribonuclease that cleaves singled stranded RNA, causes 28s rRNA fragmentation, and activates Janus Kinase (JAK), a mitochondrial-dependent apoptosis signaling molecule. Drug Indication Investigated for use/treatment in solid tumors and cancer/tumors (unspecified). Mechanism of Action 3'-C-ethynylcytidine is metabolized in tumor cells to ethynylcytidine triphosphate (ECTP), which inhibits RNA synthesis by competitive inhibition of RNA polymerases I, II and III; subsequently, RNase L is activated, resulting in apoptosis. RNase L is a potent antiviral and antiproliferative endoribonuclease that cleaves singled stranded RNA, causes 28s rRNA fragmentation, and activates Janus Kinase (JAK), a mitochondrial-dependent apoptosis signaling molecule. |
Molecular Formula |
C11H13N3O5
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Molecular Weight |
267.23802
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Exact Mass |
267.086
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CAS # |
180300-43-0
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PubChem CID |
176885
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Appearance |
White to yellow solid powder
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Density |
1.61g/cm3
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Boiling Point |
536.4ºC at 760 mmHg
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Flash Point |
278.2ºC
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Vapour Pressure |
9.56E-14mmHg at 25°C
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Index of Refraction |
1.677
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LogP |
-2.7
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Hydrogen Bond Donor Count |
4
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
3
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Heavy Atom Count |
19
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Complexity |
508
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Defined Atom Stereocenter Count |
4
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SMILES |
C#C[C@]1([C@H](O[C@H]([C@@H]1O)N2C=CC(=NC2=O)N)CO)O
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InChi Key |
JFIWEPHGRUDAJN-DYUFWOLASA-N
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InChi Code |
InChI=1S/C11H13N3O5/c1-2-11(18)6(5-15)19-9(8(11)16)14-4-3-7(12)13-10(14)17/h1,3-4,6,8-9,15-16,18H,5H2,(H2,12,13,17)/t6-,8+,9-,11-/m1/s1
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Chemical Name |
4-amino-1-[(2R,3R,4S,5R)-4-ethynyl-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
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Synonyms |
SB596168 3Ethynylcytidine; ECydTAS106TAS 1063CEthynylcytidineAIDS241582AIDS241582
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~250 mg/mL (~935.49 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.78 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.78 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.7420 mL | 18.7098 mL | 37.4195 mL | |
5 mM | 0.7484 mL | 3.7420 mL | 7.4839 mL | |
10 mM | 0.3742 mL | 1.8710 mL | 3.7420 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.