2. Apoptosis
  3. Apoptosis Caspase Bcl-2 Family
  4. Glufosfamide

Glufosfamide  (Synonyms: D 19575; Glucosylifosfamide mustard)

Cat. No.: HY-16232 Purity: ≥98.0%
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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.

For research use only. We do not sell to patients.

Glufosfamide

Glufosfamide Chemical Structure

CAS No. : 132682-98-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Solution
10 mM * 1 mL in Water In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Glufosfamide:

Glufosfamide Related Antibodies

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  • Biological Activity

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Description

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[1][2][3].

In Vitro

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.

Glufosfamide Related Antibodies

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 10, 25, 50 μM
Incubation Time: 48, 72 h
Result: Induced apoptosis frequency.
Increased the expression of caspase-9 and caspase-3.
In Vivo

Glufosfamide (3-100 mg/kg, i.v., daily, 14 days) shows dose-dependent tumor growth inhibition in MiaPaCa-2-RFP orthotopic nude mouse model[2].
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.

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]
Dosage: 3, 10, 30, 100 mg/kg
Administration: i.v. daily for 14 days
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.
Animal Model: MiaPaCa-2 cells (1 × 106) were injected intrapancreatically into nude mice after midline incision and laparotomy under isoflurane anesthesia[2]
Dosage: 10, 30 mg/kg combined with Gemcitabine (300 mg/kg, i.p., weekly)
Administration: i.v. daily for 14 days
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.
Clinical Trial
Molecular Weight

383.16

Formula

C10H21Cl2N2O7P
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O[C@@H]1[C@@H](O)[C@H](OP(NCCCl)(NCCCl)=O)O[C@H](CO)[C@H]1O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 125 mg/mL (326.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6099 mL 13.0493 mL 26.0986 mL
5 mM 0.5220 mL 2.6099 mL 5.2197 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (130.49 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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.

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Glufosfamide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Glufosfamide132682-98-5D 19575 Glucosylifosfamide mustardD19575D-19575ApoptosisCaspaseBcl-2 FamilyMiaPaCa-2-RFP mouse modelhepatocellular carcinomapancreatic carcinomaprostate cancerInhibitorinhibitorinhibit

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