Dexelvucitabine
Based on 1 Customer Validation
Dexelvucitabine (Reverset; d-d4FC), a Cytidine (HY-B0158) analog, is an orally active nucleoside reverse transcriptase inhibitor. Dexelvucitabine is a powerful agent against HIV-1-resistant viruses containing a thymidine analog and/or M184V mutation in the viral polymerase. Dexelvucitabine is a 2′-Deoxycytidine antiretroviral agent.
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- Purity: 99.52%
- CAS No.: 134379-77-4
- 화학식: C9H10FN3O3
- 분자량:227.19
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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HIV-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16 | IC50 |
>200 μM
Compound: ent-1
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In vitro inhibitory activity against growth of HIV infected B16 cell line
In vitro inhibitory activity against growth of HIV infected B16 cell line
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[PMID: 9873711] |
| CCRF-CEM | IC50 |
>100 μM
Compound: 6a
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Tested in vitro for anticancer activity against CEM cells
Tested in vitro for anticancer activity against CEM cells
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[PMID: 10072683] |
| CCRF-CEM | IC50 |
100 μM
Compound: ent-1
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In vitro inhibitory activity against growth of HIV infected CEM cell line
In vitro inhibitory activity against growth of HIV infected CEM cell line
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[PMID: 9873711] |
| CCRF-CEM | IC50 |
127 μM
Compound: ent-1
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In vitro inhibitory activity against growth of HIV infected CEM cells combined with murine CTLL-2T lymphoblast cell line
In vitro inhibitory activity against growth of HIV infected CEM cells combined with murine CTLL-2T lymphoblast cell line
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[PMID: 9873711] |
| DLD-1 | IC50 |
>200 μM
Compound: ent-1
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In vitro inhibitory activity against growth of HIV infected DLD-1 cell line
In vitro inhibitory activity against growth of HIV infected DLD-1 cell line
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[PMID: 9873711] |
| HeLa | IC50 |
>50 μM
Compound: Beta-D-dd (table 3)
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In vitro antiviral activity against HIV in HeLa CD4 cells
In vitro antiviral activity against HIV in HeLa CD4 cells
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10.1016/0960-894X(95)00472-6 |
| HepG2 | IC50 |
>100 μM
Compound: 6a
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Tested in vitro for anticancer activity against HepG2 cells
Tested in vitro for anticancer activity against HepG2 cells
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[PMID: 10072683] |
| HepG2 | IC50 |
>100 μM
Compound: Beta-D-dd (table 3)
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In vitro antiviral activity against HBV in Hep G2 cells
In vitro antiviral activity against HBV in Hep G2 cells
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10.1016/0960-894X(95)00472-6 |
| HepG2 | IC50 |
>200 μM
Compound: ent-1
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In vitro inhibitory activity against growth of HIV infected HepG2 cell line
In vitro inhibitory activity against growth of HIV infected HepG2 cell line
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[PMID: 9873711] |
| LNCaP | IC50 |
>100 μM
Compound: 6a
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Tested in vitro for anticancer activity against LNCaP cells
Tested in vitro for anticancer activity against LNCaP cells
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[PMID: 10072683] |
| MCF7 | IC50 |
>100 μM
Compound: 6a
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Tested in vitro for anticancer activity against MCF-7 cells
Tested in vitro for anticancer activity against MCF-7 cells
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[PMID: 10072683] |
| MT2 | IC50 |
100 μM
Compound: ent-1
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In vitro inhibitory activity against growth of HIV infected MT-2/IIIB cell line
In vitro inhibitory activity against growth of HIV infected MT-2/IIIB cell line
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[PMID: 9873711] |
| PC-3 | IC50 |
>10 μM
Compound: 6a
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Tested in vitro for anticancer activity against PC-3 cells
Tested in vitro for anticancer activity against PC-3 cells
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[PMID: 10072683] |
| Rat1 | IC50 |
>200 μM
Compound: ent-1
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In vitro inhibitory activity against growth of HIV infected Rat-1 cell line
In vitro inhibitory activity against growth of HIV infected Rat-1 cell line
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[PMID: 9873711] |
| SK-MEL-28 | IC50 |
>100 μM
Compound: 6a
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Tested in vitro for anticancer activity against SK-MEL-28 cells
Tested in vitro for anticancer activity against SK-MEL-28 cells
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[PMID: 10072683] |
| SK-MES-1 | IC50 |
>100 μM
Compound: 6a
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Tested in vitro for anticancer activity against SK-MES-1 cells
Tested in vitro for anticancer activity against SK-MES-1 cells
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[PMID: 10072683] |
| Vero | IC50 |
>100 μM
Compound: 6a
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Tested in vitro for cytotoxicity against Vero cells
Tested in vitro for cytotoxicity against Vero cells
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[PMID: 10072683] |
Dexelvucitabine has a favorable pharmacokinetic profile with a long half-life (4.71 and 10.75 h after administration by the intravenous [i.v.] and oral [p.o.] routes, respectively) in woodchucks[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 134379-77-4
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Appearance Solid
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분자량 227.19
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화학식 C9H10FN3O3
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Color White to off-white
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SMILES
O=C1N(C=C(C(N)=N1)F)[C@]2([H])O[C@@H](C=C2)CO
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Synonyms
Reverset; d-d4FC
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (220.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Brenda I Hernandez-Santiago, et al. Antiviral and cellular metabolism interactions between Dexelvucitabine and lamivudine. Antimicrob Agents Chemother. 2007 Jun;51(6):2130-5. [Content Brief]
[2]. L Ma, et al. Pharmacokinetics of the antiviral agent beta-D-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine in rhesus monkeys. Antimicrob Agents Chemother. 1999 Feb;43(2):381-4. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.4016 mL | 22.0080 mL | 44.0160 mL | 110.0401 mL |
| 5 mM | 0.8803 mL | 4.4016 mL | 8.8032 mL | 22.0080 mL | |
| 10 mM | 0.4402 mL | 2.2008 mL | 4.4016 mL | 11.0040 mL | |
| 15 mM | 0.2934 mL | 1.4672 mL | 2.9344 mL | 7.3360 mL | |
| 20 mM | 0.2201 mL | 1.1004 mL | 2.2008 mL | 5.5020 mL | |
| 25 mM | 0.1761 mL | 0.8803 mL | 1.7606 mL | 4.4016 mL | |
| 30 mM | 0.1467 mL | 0.7336 mL | 1.4672 mL | 3.6680 mL | |
| 40 mM | 0.1100 mL | 0.5502 mL | 1.1004 mL | 2.7510 mL | |
| 50 mM | 0.0880 mL | 0.4402 mL | 0.8803 mL | 2.2008 mL | |
| 60 mM | 0.0734 mL | 0.3668 mL | 0.7336 mL | 1.8340 mL | |
| 80 mM | 0.0550 mL | 0.2751 mL | 0.5502 mL | 1.3755 mL | |
| 100 mM | 0.0440 mL | 0.2201 mL | 0.4402 mL | 1.1004 mL |
Dexelvucitabine Related Classifications
HY-14920 Related Classifications
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