Glufosfamide
Based on 1 Customer Validation
Glufosfamide is a glucose-conjugated alkylating cytotoxic agent and a derivative of Ifosfamide (HY-17419). Glufosfamide induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in cancer cells. Glufosfamide shows great anti-tumor activity in MiaPaCa-2-RFP mouse model. Glufosfamide can be used for the study of hepatocellular carcinoma, prostate cancer and pancreatic carcinoma.
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- Pureza: 98.0%
- No. CAS: 132682-98-5
- Fòrmula: C10H21Cl2N2O7P
- Peso molecular:383.16
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Glufosfamide (10-1000 μM, 24-72 h) exhibits cytotoxicity in a concentration- and time-dependent manner in HepG2 cells, with lower IC50 values (24 h: 112.32 μM; 48 h: 83.23 μM; 72 h: 51.66 μM)[1].
Glufosfamide (10-50 μM, 48-72 h) induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in HepG2, LNCaP and PC-3 cells[1][3].
Glufosfamide (10-50 μM, 48-72 h) downregulates Bcl2 gene expression and reduces mitochondrial membrane potential and cellular ATP levels in HepG2 cells[1].
Glufosfamide (10 mg/mL, 24 h) combined with Gemcitabine (HY-17026) (1 mg/mL) shows a more significant inhibitory effect on the growth of MiaPaCa-2, H766t, and PANC-1 pancreatic cancer cells in proliferation assays compared to single-agent treatmentand induces slightly more than additive apoptosis (sub-G1 phase)[2].
Glufosfamide (0.1-300 μM, 72 h) exhibits concentration-dependent cytotoxicity in LNCaP and PC-3 prostate cancer cells, with IC50 values of 86.8 μM and 70 μM, respectively[3].
Glufosfamide (0.1-300 μM, 72 h) combined with Docetaxel (HY-B0011) down-regulates Bcl-2 expression and up-regulates Bax, caspase-3, and caspase-9 expression in LNCaP and PC-3 prostate cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:10, 25, 50 μM
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Incubation Time:48, 72 h
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Result:Induced apoptosis frequency.
Increased the expression of caspase-9 and caspase-3.
Glufosfamide (10-30 mg/kg, i.v., daily, 14 days) significantly reduces tumor volume when combined with Gemcitabine in MiaPaCa-2-RFP orthotopic nude mouse model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MiaPaCa-2 cells stably expressing red fluorescent protein (RFP) (5 × 106 in 200 µL) were subcutaneously implanted into the flanks of nude mice to generate tumor stocks[2]
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Dosage:3, 10, 30, 100 mg/kg
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Administration:i.v. daily for 14 days
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Result:Achieved dose-dependent tumor volume reduction in MiaPaCa-2-RFP orthotopic nude mouse model, with 100 mg/kg.
Significantly prolonged 50% survival at doses 30 or 100 mg/kg.
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Animal Model:MiaPaCa-2 cells (1 × 106) were injected intrapancreatically into nude mice after midline incision and laparotomy under isoflurane anesthesia[2]
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Dosage:10, 30 mg/kg combined with Gemcitabine (300 mg/kg, i.p., weekly)
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Administration:i.v. daily for 14 days
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Result:Resulted in significantly greater tumor volume reduction.
Prolonged survival in MiaPaCa-2-RFP orthotopic model.
Reduced metastatic incidence.
Enhanced apoptosis (increased TUNEL staining) and proliferation inhibition (decreased PCNA staining).
Showed no significant changes in body weights of treated mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 132682-98-5
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Appearance Solid
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Peso molecular 383.16
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Fòrmula C10H21Cl2N2O7P
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Color Off-white to light yellow
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SMILES
O[C@@H]1[C@@H](O)[C@H](OP(NCCCl)(NCCCl)=O)O[C@H](CO)[C@H]1O
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Synonyms
D 19575; Glucosylifosfamide mustard
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
H2O : 125 mg/mL (326.23 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (130.49 mM); Clear solution; Need ultrasonic
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ahmed DE, et al. An in vitro cytotoxicity of glufosfamide in HepG2 cells relative to its nonconjugated counterpart. J Egypt Natl Canc Inst. 2021 Aug 23;33(1):22. [Content Brief]
[2]. Ammons WS, et al. A novel alkylating agent, glufosfamide, enhances the activity of gemcitabine in vitro and in vivo. Neoplasia. 2007 Aug;9(8):625-33. [Content Brief]
[3]. Attia RT, et al. The chemomodulatory effects of glufosfamide on docetaxel cytotoxicity in prostate cancer cells. PeerJ. 2016 Jun 29;4:e2168. [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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.6099 mL | 13.0493 mL | 26.0986 mL | 65.2464 mL |
| 5 mM | 0.5220 mL | 2.6099 mL | 5.2197 mL | 13.0493 mL | |
| 10 mM | 0.2610 mL | 1.3049 mL | 2.6099 mL | 6.5246 mL | |
| 15 mM | 0.1740 mL | 0.8700 mL | 1.7399 mL | 4.3498 mL | |
| 20 mM | 0.1305 mL | 0.6525 mL | 1.3049 mL | 3.2623 mL | |
| 25 mM | 0.1044 mL | 0.5220 mL | 1.0439 mL | 2.6099 mL | |
| 30 mM | 0.0870 mL | 0.4350 mL | 0.8700 mL | 2.1749 mL | |
| 40 mM | 0.0652 mL | 0.3262 mL | 0.6525 mL | 1.6312 mL | |
| 50 mM | 0.0522 mL | 0.2610 mL | 0.5220 mL | 1.3049 mL | |
| 60 mM | 0.0435 mL | 0.2175 mL | 0.4350 mL | 1.0874 mL | |
| 80 mM | 0.0326 mL | 0.1631 mL | 0.3262 mL | 0.8156 mL | |
| 100 mM | 0.0261 mL | 0.1305 mL | 0.2610 mL | 0.6525 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Glufosfamide Related Classifications
HY-16232 Related Classifications
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