Temozolomide

SKU: orb1309506

Description

Temozolomide

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 85622-93-1
• MW: 194.15
• Purity: 98.97%
• Formula: C₆H₆N₆O₂
• SMILES: CN1N=NC2=C(N=CN2C1=O)C(N)=O
• Target: DNA Alkylator/Crosslinker,Apoptosis,Autophagy,DNA/RNA Synthesis
• Solubility: H2O:5 mg/mL (25.75 mM);10% DMSO+90% Saline:2.88 mg/mL (14.83 mM);DMSO:30.6 mg/mL (157.61 mM);PBS:5 mg/mL (25.75 mM)

Bioactivity

• Target IC50:
  A2058 cells:35.5 μM|CTX TNA2 cells:430.6 μM|C6 cells:34 μM|DBTRG-05MG cells:119.3 μM|IgR3 cells:22 μM|MM200 cells:23 μM|A 172 cells:6.5 x 104 nM|A431 cells:366 μM|A375 cells:> 75 μM|A549 cells:> 250 μM|SK-MEL-2 cells:> 256 μM|Astrocytes:> 1 mM|B16 F10 cells:258 μM|Mel-FH cells:> 247 μM|DLD-1 cells:> 250 μM
• In Vivo:
  METHODS: To assay antitumor activity in vivo, Temozolomide (68 mg/kg by gavage) and AG-014699 (1 mg/kg by intraperitoneal injection) were administered intraperitoneally to CD1 nu/nu mice harboring medulloblastomas D425Med, D283Med, or D384Med once daily for five days. RESULTS: AG-014699 enhanced the efficacy of Temozolomide in an in vivo model of medulloblastoma. METHODS: To assay antitumor activity in vivo, Temozolomide (0.9 mg/kg orally once daily) and Aldox (16 mg/kg intravenously once weekly) were administered to Foxn1 nude mice bearing human glioblastoma U87MG once daily for five weeks. RESULTS: Combined treatment with Temozolomide and AldoxAldo induced significant tumor volume suppression and increased survival.
• In Vitro:
  METHODS: Melanoma cells SK-mel-28, MM200, IgR3, Mel-FH were treated with Temozolomide (0-500 μM) for 72 h. Cell viability was examined using MTT. RESULTS: The p53 status and MGMT expression levels were correlated with the sensitivity of Temozolomide. MM200 and IgR3 (expressing wild-type p53 and low MGMT levels) showed comparable sensitivity to Temozolomide, with IC50 values of 23 and 22 μM, respectively, whereas SK mel-28 and Mel-FH (mutant-type p53 and high MGMT level) were resistant with IC50 values >256 and >247 μM. METHODS: Melanoma cells MM200 and IgR3 were treated with Temozolomide (100 μM) for 24-72 h. The cell cycle was examined by Flow Cytometry. RESULTS: Temozolomide induced G2/M cell cycle arrest in MM200 and IgR3 cells. METHODS: Human glioma cells U118 were treated with Temozolomide (250-500 μM) for 3-48 h. The m5C level in DNA was measured. RESULTS: The response of U118 cells to Temozolomide depends on the concentration and time of the reaction. The amount of m5C in DNA increased significantly within a short period of time after Temozolomide treatment. m5C(R) reached the highest level after 24 h of treatment with 500 μM Temozolomide.
• Cell Research:
  Cell lines exposed to TMZ (with or without 5-Aza or O6-BG pre-treatment) were grown in 24-well plates under standard culture conditions for 6 days. Cytotoxicity was determined using the sulphorhodamine-B (SRB) method. Briefly, the cells were fixed with 10% trichloroacetic acid for 20 min at 4°C then washed three times with water. After 24 hours, cells were stained for 30 min at room temperature with 0.4% SRB dissolved in 1% acetic acid and then washed three times with 1% acetic acid. The plates were air-dried and the dye solubilized with 300 ml/well of 10 mM Tris base (pH 10.5) for 10 min on a shaker. The optical density of each well was measured spectrophotometrically using a Titertek multiscan colorimeter at 492 nm .
• Animal Research:
  TZM was dissolved in dimethyl-sulfoxide (40 mg/mL), diluted in saline (5 mg/mL), and administered intraperitoneally on day 2 after tumor injection at 100 mg/kg or 200 mg/kg, doses commonly used for in vivo preclinical studies.15-17 Because cytotoxicity induced by TZM and PARP inhibitors can be improved by fractionated modality of treatment,9 in selected groups a total dose of 200 mg/kg TZM was divided in 2 doses of 100 mg/kg given on days 2 and 3. NU1025 was dissolved in polyethylene glycol-400 (40% in saline) and was injected intracranially at the maximal deliverable dose (1 mg/mouse, 0.03 mL) or, in selected groups, intraperitoneally (0.3 mL) on day 2 after tumor challenge, 1 hour before TZM administration. Control mice were injected with drug vehicles .

Storage & Handling

• Storage: store under nitrogen,keep away from direct sunlight | Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TMZ, Temozolomide, RNASynthesis, RNA Synthesis, TZM, Autophagy, Apoptosis, CCRG 81045, CCRG81045, CCRG-81045, DNASynthesis, DNA Synthesis, DNAAlkylator, DNA replication, DNA Alkylator, DNA Alkylator/Crosslinker, Crosslinker, NSC362856, NSC-362856, inhibit, NSC 362856, Inhibitor

Compound Identifiers

PubChem CID

5394