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[CAS NO. 85622-93-1]  Temozolomide

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PRODUCTS SPECIFICATIONS [85622-93-1]

Catelog
HY-17364
Brand
MCE
CAS
85622-93-1

DESCRIPTION [85622-93-1]

Overview

MDLMFCD00866492
Molecular Weight194.15
Molecular FormulaC6H6N6O2
SMILESO=C(C1=C(N2C=N1)N=NN(C)C2=O)N

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

75 Publications Citing Use of MCE


Summary

Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects [1] [2] .


IC50 & Target

DNA alkylator [1]


In Vitro

Temozolomide (TZM) is a methylating agent that crosses the blood-brain barrier and is indicated for malignant gliomas and metastatic melanomas. Temozolomide is effective against tumor cells that are characterized by low levels of O 6 -alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system (MR) [1] . Determination of the IC 50 for Temozolomide (TZM) in different cell lines gave values ranging from 14.1 to 234.6 μM that fell into two clearly differentiated groups: cell lines with low IC 50 values (<50 μM), which include A172 (14.1±1.1 μM) and LN229 cells (14.5±1.1 μM), and those with high IC 50 values (>100 μM), which include SF268 (147.2±2.1 μM) and SK-N-SH cells (234.6±2.3 μM) [3] .

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


In Vivo

Temozolomide (TZM), as a single agent, does not significantly increase mdian survival time (MST) with respect to control. Noteworthy, intracranial injection of NU1025, immediately before the administration of 100 or 200 mg/kg Temozolomide, significantly increases lifespans with respect to controls or to groups treated with Temozolomide only. When Temozolomide is fractionated, the increase in lifespan (ILS) obtained with this schedule is higher than that observed when NU1025 is combined with a single injection of Temozolomide (statistical comparison of survival curves: NU1025 intracranially+Temozolomide 100 mg/kg×2 vs NU1025+Temozolomide 200 mg/kg; P=0.023) [1] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT02015728 Seattle Children´s Hospital|Cures Within Reach
Recurrent Childhood Brain Tumor
December 2013 Not Applicable
NCT02023905 University of California, San Francisco|Novartis
Low Grade Glioma|World Health Organization (WHO) Grade II Astrocytomas|Oligodendrogliomas|Mixed Oligoastrocytomas
February 18, 2018 Phase 2
NCT00869401 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI)|Bristol-Myers Squibb
Brain and Central Nervous System Tumors
June 2009 Phase 1|Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

-20°C, protect from light, stored under nitrogen

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


Solvent & Solubility

In Vitro:

DMSO : 20.83 mg/mL ( 107.29 mM ; Need ultrasonic)

H 2 O : 2.86 mg/mL ( 14.73 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.1507 mL 25.7533 mL 51.5066 mL
5 mM 1.0301 mL 5.1507 mL 10.3013 mL
10 mM 0.5151 mL 2.5753 mL 5.1507 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 9.09 mg/mL (46.82 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

  • 2.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 1.25 mg/mL (6.44 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (6.44 mM); Clear solution

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 1.25 mg/mL (6.44 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide, 3,4-dihydro-3-methyl-4-oxo-
3,4-Dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide
CCRG 81045
NSC 362856
M and B 39831
MB 39831
Methazolastone
Temozolomide
Temodal
Sch 52365
Temodar
3-Methyl-4-oxo-8-imidazolo[5,1-d][1,2,3,5]tetrazinecarboxamide
8-Carbamoyl-3-methylimidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one
3-Methyl-8-carbamoylimidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one
3-Methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
T 2577
3-Methyl-4-oxoimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
3-Methyl-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide
3-Methyl-4-oxo-3H,4H-imidazo[4,3-d][1,2,3,5]tetrazine-8-carboxamide
Temomedac

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