Oxaliplatin [61825-94-3]

Referencia HY-17371-100mg

embalaje : 100mg

Marca : MedChemExpress

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Descripciòn

Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and induces apoptosis. Oxaliplatin can be used for cancer research[1][2][3].

IC50 & Target

IC50: DNA synthesis[1]

In Vitro

Oxaliplatin (24-72 hours; 2-128 μM; HCC, HCCLM3 and Hep3B cells) inhibits cell growth and induces apoptosis[1].
Oxaliplatin (10 μM; 15-240 mins; CEM cells ) induces primary and secondary DNA lesions, including DNA cross-links (ISC) and DNA-protein cross-links (DPC)[2].
Oxaliplatin (0.01 to 100 μM; 24 hours) potently inhibits bladder carcinoma cell lines RT4 and TCCSUP, ovarian carcinoma cell line A2780, colon carcinoma cell line HT-29, glioblastoma cell lines U-373MG and U-87MG, and melanoma cell lines SK-MEL-2 and HT-144 with IC50 of 11 μM, 15 μM, 0.17 μM, 0.97 μM, 2.95 μM, 17.6 μM, 30.9 μM and 7.85 μM, respectively[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HCC, HCCLM3 and Hep3B cells
Concentration: 24, 48 and 72 hours
Incubation Time: 2, 4, 8, 16, 32, 64 and 128 μM
Result: Decreased cell viability in a dose- and time-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HCCLM3 and Hep3B cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Increased the percentage of apoptotic cells (17.70% for HCCLM3 cells; 21.19% for Hep3B cells).

Cell Cycle Analysis[1]

Cell Line: HCCLM3 cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: Down-regulated the expression of Bcl-2 and Bcl-xL, and increased the expression of Bax.
In Vivo

Oxaliplatin (5-10 mg/kg; i.p.; for 32 days; nude mice) inhibits tumor growth[1].


Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

1. Induction of acute chemotherapy-induced peripheral neuropathy (CINP)[10][11][12]
Background
Oxaliplatin induces acute neuropathic pain through a multifaceted mechanism involving disruption of voltage-gated ion channels, activation of TRP channels, suppression of DNA transcription, mitochondrial dysfunction, and increased generation of reactive oxygen species (ROS)[10].
Specific Modeling Methods
Rats: SD rats
Administration: Oxaliplatin (3, 5, 6 and 10 mg/kg) • i.p. • once
Rats: SD rats
Administration: Oxaliplatin (2 mg/kg) • i.p. • once
Mice: Male CD-1 mice
Administration: Oxaliplatin (10 mg/kg) • i.p. • once
Mice: Male C57BL/6 mice
Administration: Oxaliplatin (3 and 6 mg/kg) • i.p. • once
Mice: Male BALB/c mice
Administration: Oxaliplatin (5 mg/kg) • i.v. • once
Note
Oxaliplatin working solution is typically prepared in 5% glucose solution.
Modeling Indicators
Molecular changes: Activation of TRPA1/TRPM8 channels, voltage-gated Na⁺ channel dysfunction, and mild ROS elevation
Mechanical allodynia: Decreased paw withdrawal threshold (Von Frey test)
Cold allodynia: Decreased paw withdrawal latency (acetone test)
Motor function: No impairment (rotarod test), confirming pain specificity

2. Induction of chronic chemotherapy-induced peripheral neuropathy (CINP)[10][11][12]
Background
Oxaliplatin-induced activation of TRPA1 channels on dorsal root ganglion (DRG) neurons triggers Ca2+ influx, leading to the accumulation of ROS, mitochondrial DNA (mtDNA) damage, disruption of the electron transport chain, and opening of the mitochondrial permeability transition pore (mPTP). These alterations subsequently impede ATP synthesis and promote neurotoxicity[10].
Specific Modeling Methods
Rats: SD rats
Administration: Oxaliplatin (2.4 mg/kg) • i.p. • on days 1-3, 6-10, and 13-15
Rats: SD rats
Administration: Oxaliplatin (2 and 4 mg/kg) • i.p. • on days 1, 2, 3, 4, 5
Rats: SD rats
Administration: Oxaliplatin (6 mg/kg) • i.p. • on days 1,3, 5, 7
Rats: SD rats
Administration: Oxaliplatin (2.4, 3.2, and 4 mg/kg) • i.p. • twice weekly for 4.5 weeks
Rats: Wistar rats
Administration: Oxaliplatin (4 mg/kg) • i.p. • twice weekly for 4 weeks
Rats: Wistar rats
Administration: Oxaliplatin (6 mg/kg) • i.p. • once per day for 6 days
Rats: SD rats
Administration: Oxaliplatin (2 mg/kg) • i.v. • once per day for 5 days
Mice: C57BL/6J mice; BALB/c mice; ICR mice
Administration: Oxaliplatin (0.3 and 3 mg/kg) • i.p. • 5 consecutive days, followed by 2 days of rest, for two cycles
Mice: C57BL/6 mice
Administration: Oxaliplatin (3 mg/kg) • i.p. • 3 times per week for 4 weeks
Mice: CD-1 mice
Administration: Oxaliplatin (2.4 mg/kg) • i.p. • 5 consecutive days each week for 2 weeks
Mice: Swiss mice
Administration: Oxaliplatin (6 mg/kg) • i.p. • every 3 days over 6 days
Note
Oxaliplatin is typically prepared in 5% glucose solution.
Modeling Indicators
Molecular changes: Increased ROS levels, activation of TLR4/NF‑κB pathway (TNF‑α, IL‑1β), decreased ATP, and TRPA1 sensitization
Histological changes: Significant loss of intraepidermal nerve fibers (IENF) in hind paw skin
Mechanical allodynia: Decreased paw withdrawal threshold (Von Frey test)
Cold allodynia: Decreased paw withdrawal latency (acetone test)
Motor function: No impairment (rotarod test), confirming pain specificity
Nerve conduction velocity: Decreased sensory nerve conduction velocity (SNCV); normal motor nerve conduction velocity (MNCV)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice[1]
Dosage: 5 and 10 mg/kg
Administration: Intraperitoneal injection; for 32 days
Result: Reduced tumor volume in HCCLM3 tumor xenografts.
Ensayo clínico
Peso molecular

397.29

Fòrmula

C8H14N2O4Pt

No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(O1)C(O[Pt]21[NH2][C@@H]3CCCC[C@H]3[NH2]2)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvente y solubilidad
In Vitro: 

H2O : 2 mg/mL (5.03 mM; ultrasonic and warming and heat to 60°C; DMSO can inactivate Oxaliplatin's activity)

DMF : 1.67 mg/mL (4.20 mM; Need ultrasonic; DMSO can inactivate Oxaliplatin's activity)

Ethanol : < 1 mg/mL (insoluble; DMSO can inactivate Oxaliplatin's activity)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5171 mL 12.5853 mL 25.1705 mL
5 mM 0.5034 mL 2.5171 mL 5.0341 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 (protect from light). 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.

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:  5% w/v Glucose Solution

    Solubility: 3.33 mg/mL (8.38 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

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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).
Pureza y Documentación
Referencias

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