Odafosfamide
Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research.
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- Purity: 99.06%
- CAS No.: 2097713-69-2
- 화학식: C21H25N4O6P
- 분자량:460.42
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보관:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Biological Activity
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AKR1C3 |
Odafosfamide (72-96 h) shows cytotoxicity against liver cancer cells (SNU-475, SNU-449, C3A, with IC50s of 15 nM, 45 nM, 5 nM, respectively) and non-small cell lung cancer cells (NSCLC) (NCI-H1944, NCI-H2228, NCIH1755, NCI-H1563, NCI-H2110, NCI-H1792, with IC50s of 2.3 nM, 0.21 nM, 8.2 nM, 2.5 nM, 1.1 nM, 4.5 nM, respectively) with high AKR1C3 protein and RNA expression levels[1].
Odafosfamide shows potent anti-leukemic activity against 19 leukemia cell lines representing B-ALL, T-ALL, and ETP-ALL (IC50s values were 60.3 nmol/L, 9.7 nmol/L, and 31.5 nmol/L, respectively)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | Vss | AUClast | T1/2 | MRT | Tmax | Cmax | AUC |
|---|---|---|---|---|---|---|---|---|---|---|
| Cynomolgus Monkey | 2 mg/kg | i.v. | 1.42 L/h/kg | 0.325 L/kg | 1459 ng·h/mL | 0.182 h | 0.232 h | / | / | / |
| Mice | 5 mg/kg | i.p. | / | / | 487 ng·h/mL | 0.0948 h | / | 0.0833 h | 1960 ng/mL | 488 ng·h/mL |
Odafosfamide (0.625-1.25 mg/kg, i.v., weekly for 2 cycles; with one week off, and another 2 cycles of weekly) inhibits tumor growth in H460 subcutaneous mice model[1].
Odafosfamide (2.5 mg/kg, 5 mg/kg, i.v., weekly for 4-5 doses) inhibits tumor growth in (CRPC) VCaP, SNU-16 and A498 xenograft mice model[1].
Odafosfamide (1.25-5 mg/kg, i.v., once a week, 3 weeks) inhibits tumor growth in PA1280, GA6201 and LU2505 xenograft mice model[1].
Odafosfamide (2.5 mg/kg, i.p., once weekly × 3 weeks) induces substantial and prolonged regressions of disease in PDX mice models of pediatric ALL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HepG2 orthotopic xenograft (~1 mm3 in diameter) female athymic nude mice (6 weeks; BALB/c-nu) model[1]
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Dosage:1.25 mg/kg, 2.5 mg/kg, 5 mg/kg
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Administration:i.v., once a week, 2 weeks
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Result:Inhibited tumor growth, with growth inhibition (TGI) at Day 34 of 52.4% at 1.25 mg/kg, 91.5% at 2.5 mg/kg and 101.2% at 5 mg/kg, respectively.
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Animal Model:(CRPC) VCaP xenograft male BALB/c nude mice model[1]
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Dosage:2.5 mg/kg, 5 mg/kg
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Administration:i.v., weekly for 5 doses
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Result:Inhibited tumor growth, with growth inhibition of 148% at 5 mg/kg, further enhanced to 158% when combined with Abiraterone (HY-70013)/Prednisolone (HY-17463).
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Animal Model:PDX (female 20–25 g) NSG mice models of pediatric ALL[2]
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Dosage:2.5 mg/kg
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Administration:i.p., once weekly × 3 weeks
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Result:Induced substantial and prolonged regressions of disease in All-8, ALL-27, ALL-29, ALL-30, ALL-31, ALL-28,ALL-AKR1C3, combined with Nelarabine (HY-13701) resulted in prolongation of mouse EFS compared with each single agent alone.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2097713-69-2
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Appearance Oil
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분자량 460.42
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화학식 C21H25N4O6P
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Color Light yellow to yellow
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SMILES
C[C@@H](C1=CC(OC2=CC(C(N(C)C)=O)=CC=C2)=C(C=C1)[N+]([O-])=O)OP(N3CC3)(N4CC4)=O
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Synonyms
(S)-OBI-3424; (S)-TH-3424; AST-3424
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (217.19 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 (5.43 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 (5.43 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 (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Meng F, et al. A novel selective AKR1C3-activated prodrug AST-3424/OBI-3424 exhibits broad anti-tumor activity. Am J Cancer Res. 2021 Jul 15;11(7):3645-3659. [Content Brief]
[2]. Evans K, et al. OBI-3424, a Novel AKR1C3-Activated Prodrug, Exhibits Potent Efficacy against Preclinical Models of T-ALL. Clin Cancer Res. 2019 Jul 15;25(14):4493-4503. [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 | 2.1719 mL | 10.8596 mL | 21.7193 mL | 54.2982 mL |
| 5 mM | 0.4344 mL | 2.1719 mL | 4.3439 mL | 10.8596 mL | |
| 10 mM | 0.2172 mL | 1.0860 mL | 2.1719 mL | 5.4298 mL | |
| 15 mM | 0.1448 mL | 0.7240 mL | 1.4480 mL | 3.6199 mL | |
| 20 mM | 0.1086 mL | 0.5430 mL | 1.0860 mL | 2.7149 mL | |
| 25 mM | 0.0869 mL | 0.4344 mL | 0.8688 mL | 2.1719 mL | |
| 30 mM | 0.0724 mL | 0.3620 mL | 0.7240 mL | 1.8099 mL | |
| 40 mM | 0.0543 mL | 0.2715 mL | 0.5430 mL | 1.3575 mL | |
| 50 mM | 0.0434 mL | 0.2172 mL | 0.4344 mL | 1.0860 mL | |
| 60 mM | 0.0362 mL | 0.1810 mL | 0.3620 mL | 0.9050 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2715 mL | 0.6787 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2172 mL | 0.5430 mL |
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