Cat. No.: HY-17364

Temozolomide

(Synonyms: NSC 362856; CCRG 81045; TMZ)

193 Cited Publications

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Based on 193 publication(s) in Google Scholar

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.

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

Purity: 99.65%
CAS No.: 85622-93-1
Formula: C₆H₆N₆O₂
Molecular Weight:194.15

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)

Temozolomide Chemical Structure

CAS No.: 85622-93-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (193)
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Biological Activity

Description

IC₅₀ & Target

DNA alkylator^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A 172	IC₅₀	6.5 x 10⁴ nM Compound: Temozolamide	Antiproliferative activity against human A172 cells after 5 days by MTT assay Antiproliferative activity against human A172 cells after 5 days by MTT assay	[PMID: 22608389]
A 172	IC₅₀	>40 μM Compound: TMZ	Cytotoxicity against human A 172 cells assessed as cell viability measured after 96 hrs by XTT assay Cytotoxicity against human A 172 cells assessed as cell viability measured after 96 hrs by XTT assay	[PMID: 34507011]
A2058	IC₅₀	35.5 μM Compound: 1, TMZ	Chemosensitization of human A2058 cells after 5 days by MTT assay Chemosensitization of human A2058 cells after 5 days by MTT assay	[PMID: 23895620]
A2780	IC₅₀	183 μM Compound: Temozolomide	Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 2 Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 2	[PMID: 11063605]
A2780	IC₅₀	188 μM Compound: Temozolomide	Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 1 Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 1	[PMID: 11063605]
A2780	IC₅₀	368 μM Compound: Temozolomide	Potentiation of growth inhibition of A2780 cells by compound alone in experiment 2 Potentiation of growth inhibition of A2780 cells by compound alone in experiment 2	[PMID: 11063605]
A2780	IC₅₀	525 μM Compound: Temozolomide	Potentiation of growth inhibition of A2780 by compound alone in experiment 1 Potentiation of growth inhibition of A2780 by compound alone in experiment 1	[PMID: 11063605]
A2780	IC₅₀	>250 μM Compound: 1, TMZ	Chemosensitization of human A2780 cells after 5 days by MTT assay Chemosensitization of human A2780 cells after 5 days by MTT assay	[PMID: 23895620]
A2780	IC₅₀	8.5 μM Compound: 1, TMZ	Chemosensitization of human A2780 cells after 5 days by MTT assay in presence of MGMT inactivator PaTrin2 Chemosensitization of human A2780 cells after 5 days by MTT assay in presence of MGMT inactivator PaTrin2	[PMID: 23895620]
A2780	IC₅₀	>250 μM Compound: 1, TMZ	Cytotoxicity against human A2780 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin2 Cytotoxicity against human A2780 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin2	[PMID: 24900418]
A-375	IC₅₀	>75 μM Compound: TMZ	Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34795855]
A-431	IC₅₀	366 μM Compound: TEM	Antiproliferative activity in human A431 Cells after 72 hrs by SRB assay Antiproliferative activity in human A431 Cells after 72 hrs by SRB assay	[PMID: 28494256]
A549	IC₅₀	>250 μM Compound: 1, TMZ	Cytotoxicity against human A549 cells after 5 days by MTT assay Cytotoxicity against human A549 cells after 5 days by MTT assay	[PMID: 24900418]
Astrocyte	IC₅₀	>1 mM Compound: Temozolamide	Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay	[PMID: 22608389]
Astrocyte	IC₅₀	>1 x 10⁶ nM Compound: Temozolamide	Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay	[PMID: 22608389]
Astrocyte	EC₅₀	51.8 μM Compound: 3, TMZ	Cytotoxicity against Rattus norvegicus Sprague-Dawley (rat) astrocytes after 4 days by cresylecth violet-staining method Cytotoxicity against Rattus norvegicus Sprague-Dawley (rat) astrocytes after 4 days by cresylecth violet-staining method	10.1007/s00044-010-9356-8
B16-F10	IC₅₀	258 μM Compound: Temozolomide	Growth inhibition of mouse B16F10 cells after 72 hrs by MTT assay Growth inhibition of mouse B16F10 cells after 72 hrs by MTT assay	[PMID: 22809560]
B16-F10	IC₅₀	>75 μM Compound: Temozolomide	Cytotoxicity against mouse B16F10 cells after 72 hrs by MTS assay Cytotoxicity against mouse B16F10 cells after 72 hrs by MTS assay	[PMID: 28602669]
B16-F10	IC₅₀	>75 μM Compound: TMZ	Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34795855]
C6	IC₅₀	34 μM Compound: Temozolomide	Cytotoxicity against rat C6 cells incubated for 48 hrs by MTT assay Cytotoxicity against rat C6 cells incubated for 48 hrs by MTT assay	[PMID: 23069682]
C6	IC₅₀	60.46 μM Compound: TMZ	Inhibition of cell proliferation of rat C6 cells assessed as cell viability after 72 hrs by sulforhodamine B assay Inhibition of cell proliferation of rat C6 cells assessed as cell viability after 72 hrs by sulforhodamine B assay	[PMID: 25442304]
C6	EC₅₀	60.46 μM Compound: TMZ	Antiproliferative activity against rat C6 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against rat C6 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 31978780]
C6	IC₅₀	>30 μM Compound: TMZ	Antiproliferative activity against rat C6 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against rat C6 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34656900]
C6	EC₅₀	16.5 μM Compound: 3, TMZ	Cytotoxicity against Rattus norvegicus (rat) C6 cells after 4 days by cresylecth violet-staining method Cytotoxicity against Rattus norvegicus (rat) C6 cells after 4 days by cresylecth violet-staining method	10.1007/s00044-010-9356-8
carcinoma cell line	IC₅₀	91 μM Compound: 1	Antitumor activity against human NCI ovarian carcinoma cell line panel Antitumor activity against human NCI ovarian carcinoma cell line panel	[PMID: 15615536]
COLO 205	IC₅₀	343 μM Compound: Temozolomide	Cytotoxicity of compound in COLO 205 cell line Cytotoxicity of compound in COLO 205 cell line	[PMID: 11063604]
CTX TNA2	IC₅₀	430.6 μM Compound: TMZ	Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32960603]
CTX TNA2	IC₅₀	486.9 μM Compound: TMZ	Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 32960603]
CTX TNA2	IC₅₀	666.4 μM Compound: TMZ	Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against rat CTX TNA2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32960603]
DBTRG-05MG	IC₅₀	119.3 μM Compound: TMZ	Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32960603]
DBTRG-05MG	IC₅₀	354.7 μM Compound: TMZ	Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 32960603]
DBTRG-05MG	IC₅₀	973.9 μM Compound: TMZ	Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human DBTRG-05MG cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32960603]
DLD-1	IC₅₀	>250 μM Compound: 1, TMZ	Cytotoxicity against human DLD1 cells after 5 days by MTT assay Cytotoxicity against human DLD1 cells after 5 days by MTT assay	[PMID: 24900418]
DLD-1	GI₅₀	>500 μM Compound: 1; TMZ	Growth inhibition of human DLD1 cells harboring hMSH6 mutation Growth inhibition of human DLD1 cells harboring hMSH6 mutation	10.1039/C6MD00384B
GL261	IC₅₀	>100 μM Compound: TMZ	Cytotoxicity against mouse GL261 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse GL261 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 30939350]
H4	IC₅₀	>100 μM Compound: TMZ	Antiproliferative activity against human H4 cells after 48 hrs by MTT assay Antiproliferative activity against human H4 cells after 48 hrs by MTT assay	[PMID: 26651221]
H4	IC₅₀	47.9 μM Compound: Temozolomide	Antiproliferative activity against human H4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human H4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38377560]
HaCaT	IC₅₀	>75 μM Compound: TMZ	Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34795855]
HCT-116	IC₅₀	4.34 μM Compound: Temozolomide	Cytotoxicity against human HCT116 cells after 4 days Cytotoxicity against human HCT116 cells after 4 days	[PMID: 19800803]
HCT-116	IC₅₀	>250 μM Compound: 1, TMZ	Chemosensitization of human HCT116 cells after 5 days by MTT assay Chemosensitization of human HCT116 cells after 5 days by MTT assay	[PMID: 23895620]
HCT-116	IC₅₀	>250 μM Compound: 1, TMZ	Cytotoxicity against human HCT116 cells after 5 days by MTT assay Cytotoxicity against human HCT116 cells after 5 days by MTT assay	[PMID: 24900418]
HCT-116	IC₅₀	<50 μM Compound: 157	Anticancer activity against human HCT-116 cells assessed as reduction in cell viability Anticancer activity against human HCT-116 cells assessed as reduction in cell viability	[PMID: 33445154]
HCT-116	GI₅₀	291 μM Compound: 1a; TMZ	Antiproliferative activity against MMR-deficient human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against MMR-deficient human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 37262998]
HCT-116	GI₅₀	>500 μM Compound: 1; TMZ	Growth inhibition of human HCT116 cells harboring hMLH1 mutation Growth inhibition of human HCT116 cells harboring hMLH1 mutation	10.1039/C6MD00384B
HeLa	GI₅₀	>50 μM Compound: TMZ	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 to 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 to 48 hrs by MTT assay	[PMID: 24986661]
HepG2	IC₅₀	5.9 μM Compound: Temozolomide	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by CCK-8 assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by CCK-8 assay	[PMID: 37335557]
Hs 683	IC₅₀	956 μM Compound: Temozolomide	Growth inhibition of human Hs683 cells after 72 hrs by MTT assay Growth inhibition of human Hs683 cells after 72 hrs by MTT assay	[PMID: 22809560]
Hs 683	IC₅₀	47.18 μM Compound: Temozolomide	Antiproliferative activity against human Hs 683 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human Hs 683 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38377560]
HT-29	IC₅₀	951 μM Compound: Temozolomide	Cytotoxicity of compound in HT-29 cell line Cytotoxicity of compound in HT-29 cell line	[PMID: 11063604]
HT-29	IC₅₀	>250 μM Compound: 1, TMZ	Cytotoxicity against human HT-29 cells after 5 days by MTT assay Cytotoxicity against human HT-29 cells after 5 days by MTT assay	[PMID: 24900418]
K562	IC₅₀	156.1 μM Compound: TEM	Cytotoxic effect in K562 cells Cytotoxic effect in K562 cells	[PMID: 12951113]
LN-18	IC₅₀	3.9 x 10⁵ nM Compound: Temozolamide	Antiproliferative activity against human LN18 cells after 5 days by MTT assay Antiproliferative activity against human LN18 cells after 5 days by MTT assay	[PMID: 22608389]
LN-229	IC₅₀	67.81 μM Compound: TMZ	Cytotoxicity effect against human LN-229 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay Cytotoxicity effect against human LN-229 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay	[PMID: 34304559]
LN-229	IC₅₀	>1000 μM Compound: TMZ	Anticancer activity against human LN-229 cells assessed as cell growth inhibition inhibition incubated for 3 days Anticancer activity against human LN-229 cells assessed as cell growth inhibition inhibition incubated for 3 days	[PMID: 37201660]
LN-229	IC₅₀	54.08 μM Compound: Temozolomide	Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38377560]
LN-229	IC₅₀	>500 μM Compound: Temozolomide	Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth incubated for 68 hrs by CCK-8 assay Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth incubated for 68 hrs by CCK-8 assay	[PMID: 39213937]
LoVo	IC₅₀	595 μM Compound: Temozolomide	Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line	[PMID: 12408707]
MCF7	IC₅₀	800 μM Compound: Temozolomide	Inhibitory concentration of compound against Mer+ breast tumor cell line MCF-7 Inhibitory concentration of compound against Mer+ breast tumor cell line MCF-7	[PMID: 11055348]
MDA-MB-231	IC₅₀	14.4 μM Compound: Temozolomide	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by CCK-8 assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by CCK-8 assay	[PMID: 37335557]
MDA-MB-238	IC₅₀	>100 μM Compound: TMZ	Cytotoxicity against human MDA-MB-238 cells assessed as cell viability measured after 96 hrs by XTT assay Cytotoxicity against human MDA-MB-238 cells assessed as cell viability measured after 96 hrs by XTT assay	[PMID: 34507011]
MDA-MB-436	IC₅₀	120 μM Compound: TMZ	Growth inhibition of human MDA-MB-436 cells after 72 hrs by SRB assay Growth inhibition of human MDA-MB-436 cells after 72 hrs by SRB assay	[PMID: 24388690]
MDCK	IC₅₀	>1000 μM Compound: TMZ	Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay	[PMID: 27823879]
MDCK	IC₅₀	775 μM Compound: TMZ	Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under normoxic condition by Alamar blue assay	[PMID: 27823879]
MDCK	IC₅₀	>1000 μM Compound: TMZ	Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay	[PMID: 27823879]
MDCK	IC₅₀	1 mM Compound: TMZ	Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 72 hrs under hypoxic condition by Alamar blue assay	[PMID: 27823879]
NCI	IC₅₀	100 μM Compound: 1	Antitumor activity against human NCI breast cancer cell line panel Antitumor activity against human NCI breast cancer cell line panel	[PMID: 15615536]
NCI	IC₅₀	100 μM Compound: 1	Antitumor activity against human NCI colon cancer cell line panel Antitumor activity against human NCI colon cancer cell line panel	[PMID: 15615536]
NCI	IC₅₀	100 μM Compound: 1	Antitumor activity against human NCI prostate cancer cell line panel Antitumor activity against human NCI prostate cancer cell line panel	[PMID: 15615536]
NCI	IC₅₀	79 μM Compound: 1	Antitumor activity against human NCI leukemia cell line panel Antitumor activity against human NCI leukemia cell line panel	[PMID: 15615536]
NCI	IC₅₀	93 μM Compound: 1	Antitumor activity against human NCI CNS cancer cell line panel Antitumor activity against human NCI CNS cancer cell line panel	[PMID: 15615536]
NCI	IC₅₀	98 μM Compound: 1	Antitumor activity against human NCI renal cancer cell line panel Antitumor activity against human NCI renal cancer cell line panel	[PMID: 15615536]
NCI	IC₅₀	98 μM Compound: 1	Antitumor activity against NCI human melanoma cell line panel Antitumor activity against NCI human melanoma cell line panel	[PMID: 15615536]
NCI-H1299	IC₅₀	>100 μM Compound: TMZ	Cytotoxicity against human NCI-H1299 cells assessed as cell viability measured after 96 hrs by XTT assay Cytotoxicity against human NCI-H1299 cells assessed as cell viability measured after 96 hrs by XTT assay	[PMID: 34507011]
Non-small cell lung cancer cell line	IC₅₀	100 μM Compound: 1	Antitumor activity against human NCI non-small cell lung cancer cell line panel Antitumor activity against human NCI non-small cell lung cancer cell line panel	[PMID: 15615536]
PANC-1	IC₅₀	>250 μM Compound: 1, TMZ	Cytotoxicity against human PANC1 cells after 5 days by MTT assay Cytotoxicity against human PANC1 cells after 5 days by MTT assay	[PMID: 24900418]
Panel NCI-60 (60 carcinoma cell lines)	GI₅₀	>100 μM Compound: 1; TMZ	Growth inhibition of human NCI60 cells after 48 hrs by MTT assay Growth inhibition of human NCI60 cells after 48 hrs by MTT assay	10.1039/C6MD00384B
Panel NCI-60 cells	GI₅₀	>100 μM Compound: 1; TMZ	Growth inhibition of human NCI60 cells after 48 hrs by MTT assay Growth inhibition of human NCI60 cells after 48 hrs by MTT assay	10.1039/C6MD00384B
Raji	IC₅₀	175 μM Compound: 1	In vitro cytotoxicity against Raji cell line In vitro cytotoxicity against Raji cell line	[PMID: 7739008]
RG2	IC₅₀	106.7 μM Compound: TMZ	Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32960603]
RG2	IC₅₀	348.2 μM Compound: TMZ	Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 32960603]
RG2	IC₅₀	962.5 μM Compound: TMZ	Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against rat RG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32960603]
SF-268	GI₅₀	>100 μM Compound: Temozolomide	Growth inhibition of human SF-268 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human SF-268 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
SF-295	GI₅₀	>100 μM Compound: Temozolomide	Growth inhibition of human SF-295 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human SF-295 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
SH-SY5Y	IC₅₀	>100 μM Compound: TMZ	Antiproliferative activity against human SH-SY5Y cells after 48 hrs by MTT assay Antiproliferative activity against human SH-SY5Y cells after 48 hrs by MTT assay	[PMID: 26651221]
SH-SY5Y	IC₅₀	>50 μM Compound: Temozolomide	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29789258]
SH-SY5Y	IC₅₀	393 μM Compound: TMZ	Cytotoxicity against human SH-SY5Y cells using best fit nonlinear regression analysis Cytotoxicity against human SH-SY5Y cells using best fit nonlinear regression analysis	[PMID: 35044783]
SH-SY5Y	IC₅₀	512.62 μM Compound: TMZ	Cytotoxicity against human SH-SY5Y cells assessed as cell viability using raw interpretation method Cytotoxicity against human SH-SY5Y cells assessed as cell viability using raw interpretation method	[PMID: 35044783]
SNB-19	IC₅₀	>250 μM Compound: 1, TMZ	Chemosensitization of human SNB19 cells expressing MGMT after 5 days by MTT assay Chemosensitization of human SNB19 cells expressing MGMT after 5 days by MTT assay	[PMID: 23895620]
SNB-19	IC₅₀	37 μM Compound: 1, TMZ	Chemosensitization of MGMT-deficient human SNB19 cells after 5 days by MTT assay Chemosensitization of MGMT-deficient human SNB19 cells after 5 days by MTT assay	[PMID: 23895620]
SNB-19	GI₅₀	35.7 μM Compound: 1; TMZ	Growth inhibition of vehicle-transfected human SNB19 cells after 7 days by MTT assay Growth inhibition of vehicle-transfected human SNB19 cells after 7 days by MTT assay	[PMID: 30108945]
SNB-19	GI₅₀	470 μM Compound: 1; TMZ	Growth inhibition of MGMT-transfected human SNB19 cells expressing MGMT after 7 days by MTT assay Growth inhibition of MGMT-transfected human SNB19 cells expressing MGMT after 7 days by MTT assay	[PMID: 30108945]
SNB-19	IC₅₀	69.87 μM Compound: TMZ	Cytotoxicity effect against human SNB-19 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay Cytotoxicity effect against human SNB-19 cells assessed as cell growth inhibition incubated for 48 hrs by trypan blue exclusion assay	[PMID: 34304559]
SNB-19	GI₅₀	>100 μM Compound: Temozolomide	Growth inhibition of human SNB-19 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human SNB-19 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
SNB-19	GI₅₀	45.6 μM Compound: 1; TMZ	Growth inhibition of empty vector transfected human SNB19 cells after 7 days by MTT assay Growth inhibition of empty vector transfected human SNB19 cells after 7 days by MTT assay	10.1039/C6MD00384B
SNB-19	GI₅₀	526 μM Compound: 1; TMZ	Growth inhibition of MGMT-transfected human SNB19 cells after 7 days by MTT assay Growth inhibition of MGMT-transfected human SNB19 cells after 7 days by MTT assay	10.1039/C6MD00384B
T98G	IC₅₀	5.7 x 10⁵ nM Compound: Temozolamide	Antiproliferative activity against human T98G cells after 5 days by MTT assay Antiproliferative activity against human T98G cells after 5 days by MTT assay	[PMID: 22608389]
T98G	IC₅₀	879 μM Compound: Temozolomide	Growth inhibition of human T98G cells after 72 hrs by MTT assay Growth inhibition of human T98G cells after 72 hrs by MTT assay	[PMID: 22809560]
T98G	GI₅₀	375 μM Compound: TMZ	Antiproliferative activity against human T98G cells assessed as cell growth inhibition incubated for 96 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human T98G cells assessed as cell growth inhibition incubated for 96 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 34731767]
T98G	IC₅₀	151 μM Compound: TMZ	Antiproliferative activity against human T98G cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human T98G cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37967166]
TLX-5	IC₅₀	5 μM Compound: 1	In vitro cytotoxicity against mouse TLX5 lymphoma cells In vitro cytotoxicity against mouse TLX5 lymphoma cells	[PMID: 7739008]
U138-MG	IC₅₀	26 μM Compound: Temozolomide	Cytotoxicity against human U138MG cells incubated for 48 hrs by MTT assay Cytotoxicity against human U138MG cells incubated for 48 hrs by MTT assay	[PMID: 23069682]
U-251	IC₅₀	>250 μM Compound: 1, TMZ	Cytotoxicity against human U251 cells after 5 days by MTT assay Cytotoxicity against human U251 cells after 5 days by MTT assay	[PMID: 24900418]
U-251	IC₅₀	>200 μM Compound: TMZ	Inhibition of cell proliferation of human U251 cells assessed as cell viability after 72 hrs by sulforhodamine B assay Inhibition of cell proliferation of human U251 cells assessed as cell viability after 72 hrs by sulforhodamine B assay	[PMID: 25442304]
U-251	IC₅₀	>100 μM Compound: TMZ	Antiproliferative activity against human U251 cells after 48 hrs by MTT assay Antiproliferative activity against human U251 cells after 48 hrs by MTT assay	[PMID: 26651221]
U-251	IC₅₀	455 μM Compound: TMZ	Cytotoxicity against human U251MG cells assessed as reduction in cell survival measured after 72 hrs by MTT assay Cytotoxicity against human U251MG cells assessed as reduction in cell survival measured after 72 hrs by MTT assay	[PMID: 30975504]
U-251	IC₅₀	36.4 μM Compound: Temozolomide	Cytotoxicity against human U251 cells incubated for 24 hrs by MTT assay Cytotoxicity against human U251 cells incubated for 24 hrs by MTT assay	[PMID: 31891260]
U-251	EC₅₀	>200 μM Compound: TMZ	Antiproliferative activity against human U251MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human U251MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 31978780]
U-251	IC₅₀	36.4 μM Compound: TMZ	Cytotoxicity against human U-251 cells by MTT assay Cytotoxicity against human U-251 cells by MTT assay	[PMID: 33915258]
U-251	IC₅₀	12.74 μM Compound: TMZ	Cytotoxicity against human U-251MG cells assessed as decrease in cell viability incubated for 6 days by alamar blue assay Cytotoxicity against human U-251MG cells assessed as decrease in cell viability incubated for 6 days by alamar blue assay	[PMID: 34384944]
U-251	IC₅₀	6.426 μM Compound: TMZ	Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 30 secs followed by incubated with compound for 6 days by alamar blue assay Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 30 secs followed by incubated with compound for 6 days by alamar blue assay	[PMID: 34384944]
U-251	IC₅₀	7.284 μM Compound: TMZ	Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 15 secs followed by incubated with compound for 6 days by alamar blue assay Cytotoxicity against cold atmospheric plasma (CAP)-treated human U-251MG cells assessed as decrease in cell viability treated with CAP for 15 secs followed by incubated with compound for 6 days by alamar blue assay	[PMID: 34384944]
U-251	IC₅₀	>30 μM Compound: TMZ	Antiproliferative activity against human U-251 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-251 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34656900]
U-251	GI₅₀	>100 μM Compound: Temozolomide	Growth inhibition of human U-251 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human U-251 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
U-251	IC₅₀	>500 μM Compound: TMZ	Anticancer activity against human U-251 cells assessed as cell growth inhibition inhibition incubated for 3 days Anticancer activity against human U-251 cells assessed as cell growth inhibition inhibition incubated for 3 days	[PMID: 37201660]
U-251	IC₅₀	>50 μM Compound: TMZ	Antiproliferative activity against human U-251 cells assessed as cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human U-251 cells assessed as cell viability measured after 72 hrs by MTT assay	[PMID: 37385078]
U-251	IC₅₀	189 μM Compound: TMZ	Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37967166]
U-251	IC₅₀	43.51 μM Compound: Temozolomide	Antiproliferative activity against human U-251MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human U-251MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38377560]
U-251	IC₅₀	>50 μM Compound: TMZ	Antiproliferative activity against human U-251 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human U-251 cells incubated for 48 hrs by MTT assay	[PMID: 38784471]
U-373MG ATCC	IC₅₀	220 μM Compound: Temozolomide	Growth inhibition of human U373 cells after 72 hrs by MTT assay Growth inhibition of human U373 cells after 72 hrs by MTT assay	[PMID: 22809560]
U-373MG ATCC	GI₅₀	369 μM Compound: 1; TMZ	Growth inhibition of MGMT-transfected human U373 cells expressing MGMT after 7 days by MTT assay Growth inhibition of MGMT-transfected human U373 cells expressing MGMT after 7 days by MTT assay	[PMID: 30108945]
U-373MG ATCC	GI₅₀	68 μM Compound: 1; TMZ	Growth inhibition of vehicle-transfected human U373 cells after 7 days by MTT assay Growth inhibition of vehicle-transfected human U373 cells after 7 days by MTT assay	[PMID: 30108945]
U-373MG ATCC	GI₅₀	395 μM Compound: 1; TMZ	Growth inhibition of MGMT-transfected human U373 cells after 7 days by MTT assay Growth inhibition of MGMT-transfected human U373 cells after 7 days by MTT assay	10.1039/C6MD00384B
U-373MG ATCC	GI₅₀	72.9 μM Compound: 1; TMZ	Growth inhibition of empty vector transfected human U373 cells after 7 days by MTT assay Growth inhibition of empty vector transfected human U373 cells after 7 days by MTT assay	10.1039/C6MD00384B
U-87MG ATCC	IC₅₀	4.9 x 10⁴ nM Compound: Temozolamide	Antiproliferative activity against human U87 cells after 5 days by MTT assay Antiproliferative activity against human U87 cells after 5 days by MTT assay	[PMID: 22608389]
U-87MG ATCC	IC₅₀	>200 μM Compound: TMZ	Inhibition of cell proliferation of human U87MG cells assessed as cell viability after 72 hrs by sulforhodamine B assay Inhibition of cell proliferation of human U87MG cells assessed as cell viability after 72 hrs by sulforhodamine B assay	[PMID: 25442304]
U-87MG ATCC	IC₅₀	>50 μM Compound: Temozolomide	Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29789258]
U-87MG ATCC	EC₅₀	>200 μM Compound: TMZ	Antiproliferative activity against human U87MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human U87MG cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 31978780]
U-87MG ATCC	IC₅₀	1.1 mM Compound: Temozolomide	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay	[PMID: 32186874]
U-87MG ATCC	IC₅₀	1.1 x 10⁶ nM Compound: Temozolomide	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay	[PMID: 32186874]
U-87MG ATCC	IC₅₀	6.4 x 10⁵ nM Compound: Temozolomide	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under normoxia condition by MTT assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs under normoxia condition by MTT assay	[PMID: 32186874]
U-87MG ATCC	IC₅₀	>200 μM Compound: TMZ	Cytotoxicity against human U-87 MG cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Cytotoxicity against human U-87 MG cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 34534673]
U-87MG ATCC	IC₅₀	>30 μM Compound: TMZ	Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 34656900]
U-87MG ATCC	IC₅₀	2898 μM Compound: TMZ	Cytotoxicity against human U-87 MG cells using best fit nonlinear regression analysis Cytotoxicity against human U-87 MG cells using best fit nonlinear regression analysis	[PMID: 35044783]
U-87MG ATCC	IC₅₀	3186 μM Compound: TMZ	Cytotoxicity against human U-87 MG cells assessed as cell viability using raw interpretation method Cytotoxicity against human U-87 MG cells assessed as cell viability using raw interpretation method	[PMID: 35044783]
U-87MG ATCC	IC₅₀	>50 μM Compound: TMZ	Antiproliferative activity against human U87 cells assessed as cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as cell viability measured after 72 hrs by MTT assay	[PMID: 37385078]
U-87MG ATCC	IC₅₀	203 μM Compound: TMZ	Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37967166]
U-87MG ATCC	IC₅₀	>200 μM Compound: TMZ	Cytotoxicity against human U-87 MG cells incubated for 48 hrs by CCK8 assay Cytotoxicity against human U-87 MG cells incubated for 48 hrs by CCK8 assay	[PMID: 39136241]
U-87MG ATCC	IC₅₀	113.36 μM Compound: Temozolomide	Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 68 hrs by CCK-8 assay Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 68 hrs by CCK-8 assay	[PMID: 39213937]
U-87MG ATCC	IC₅₀	19.38 μM Compound: Temozolomide	Cytotoxicity against human U87 cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human U87 cells assessed as growth inhibition after 72 hrs by SRB assay	10.1039/C4MD00264D
WiDr	IC₅₀	1720 μM Compound: temozolomide	Cytotoxicity against human WiDr cells overexpressing MGMT after 48 hrs by trypan blue staining-based hemocytometric analysis Cytotoxicity against human WiDr cells overexpressing MGMT after 48 hrs by trypan blue staining-based hemocytometric analysis	[PMID: 25874335]
WM 266-4	IC₅₀	>100 μM Compound: TMZ	Cytotoxicity against human WM 266-4 cells assessed as cell viability measured after 96 hrs by XTT assay Cytotoxicity against human WM 266-4 cells assessed as cell viability measured after 96 hrs by XTT assay	[PMID: 34507011]

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 O⁶-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system (MR)^[1]. Determination of the IC₅₀ 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 IC₅₀ values (<50 μM), which include A172 (14.1±1.1 μM) and LN229 cells (14.5±1.1 μM), and those with high IC₅₀ values (>100 μM), which include SF268 (147.2±2.1 μM) and SK-N-SH cells (234.6±2.3 μM)^[3].

MedChemExpress (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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 85622-93-1
Appearance Solid
Molecular Weight 194.15
Formula C₆H₆N₆O₂
Color White to yellow
SMILES

O=C(C1=C(N2C=N1)N=NN(C)C2=O)N
Synonyms

NSC 362856; CCRG 81045; TMZ
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)

Publications (193)

All WBCell Proliferation/Viability AssayIFIHC

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Cancer Cell

Long-range cholinergic input promotes glioblastoma progression. [Abstract]

2025 Aug 12:S1535-6108(25)00330-7. PMID: 40829591
Nat Photonics

2024 Jan 18.
Cancer Commun (Lond)

2025 Dec 26.
Nat Cell Biol

Tumour microenvironment programming by an RNA-RNA-binding protein complex creates a druggable vulnerability in IDH-wild-type glioblastoma. [Abstract]

2024 Jun;26(6):1003-1018. PMID: 38858501
Cancer Res

ETC-501 is a Brain Penetrant MNK Kinase Inhibitor that Potentiates TMZ-Induced Senescence and Sensitizes Glioblastoma Cells to Senolytic Therapy. [Abstract]

2026 Jan 22. PMID: 41570320
Cell Death Differ

Hypoxia-induced GLT8D1 promotes glioma stem cell maintenance by inhibiting CD133 degradation through N-linked glycosylation. [Abstract]

2022 Sep;29(9):1834-1849. PMID: 35301431
Acta Pharm Sin B

DDAH1 promotes neurogenesis and neural repair in cerebral ischemia. [Abstract]

2024 May;14(5):2097-2118. PMID: 38799640

Temozolomide purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2024 May;14(5):2097-2118. [Abstract]

Temozolomide (TMZ) (25 mg/kg; i.p.; administered during the first 3 days of each week for 4 weeks during reperfusion) significantly reduces the levels of synaptic-associated proteins including synaptophysin, PSD95, and GAP43 in wild-type mice subjected to MCAO.
Adv Sci (Weinh)

Low YTHDC1 Expression Upregulates FSCN1 to Promote Nuclear F-Actin Formation and Facilitate Double-strand DNA Breaks Repair in TMZ-Resistant Glioblastoma. [Abstract]

2025 Dec 27:e13632. PMID: 41454694
Adv Sci (Weinh)

Sanggenol L Enhances Temozolomide Drug Sensitivity by Inhibiting Mitophagy and Inducing Apoptosis Through the Regulation of the TRIM16-OPTN Axis in Glioblastoma. [Abstract]

2025 Sep 24:e02915. PMID: 40990506
Adv Sci (Weinh)

A Novel Class of Multi-substituted Diaryl Scaffold Derivatives Inhibit Glioblastoma Progression by Targeting CD155. [Abstract]

2025 Jun 10:e06688. PMID: 40492418
Adv Sci (Weinh)

Histone H3K9 Lactylation Confers Temozolomide Resistance in Glioblastoma via LUC7L2-Mediated MLH1 Intron Retention. [Abstract]

2024 May;11(19):e2309290. PMID: 38477507

Temozolomide purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 May;11(19):e2309290. [Abstract]

Temozolomide (TMZ) (5 mg/kg; orally gavaged once daily for 4 weeks) increases the levels of pan Kla and H3K9la in BALB/C mice with GBM xenografts.
Adv Sci (Weinh)

Kinome-Wide Synthetic Lethal Screen Identifies PANK4 as a Modulator of Temozolomide Resistance in Glioblastoma. [Abstract]

2024 Apr;11(15):e2306027. PMID: 38353396

Temozolomide purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Apr;11(15):e2306027. [Abstract]

Temozolomide (TMZ) (1.5 mg/kg; i.p., every other day for 12 days) combined with PANK4 knockdown significantly reduces the expression of the tumor proliferation marker Ki-67 in T98GRes xenograft mice.
Neuro Oncol

Targeting PDGFRα-activated glioblastoma through specific inhibition of SHP-2-mediated signaling. [Abstract]

2019 Nov 4;21(11):1423-1435. PMID: 31232447
Theranostics

Molecular signatures of BRCAness analysis identifies PARP inhibitor Niraparib as a novel targeted therapeutic strategy for soft tissue Sarcomas. [Abstract]

2020 Jul 25;10(21):9477-9494. PMID: 32863940

Temozolomide purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 25;10(21):9477-9494. [Abstract]

Temozolomide (TMZ) (10 μM; 14 d) synergistically inhibits proliferation in STS cell lines when combined with MK4827 (HY-10619) (0.5 μM; 14 d).
Exp Mol Med

Trametinib activates endogenous neurogenesis and recovers neuropathology in a model of Alzheimer's disease. [Abstract]

2023 Oct;55(10):2177-2189. PMID: 37779138
J Exp Clin Cancer Res

Protein disulfide-isomerase A4 confers glioblastoma angiogenesis promotion capacity and resistance to anti-angiogenic therapy. [Abstract]

2023 Mar 30;42(1):77. PMID: 36997943
J Exp Clin Cancer Res

HDAC6 involves in regulating the lncRNA-microRNA-mRNA network to promote the proliferation of glioblastoma cells. [Abstract]

2022 Feb 2;41(1):47. PMID: 35109908
J Nanobiotechnology

Recruiting T-cells toward the brain for enhanced glioblastoma chemo-immunotherapy efficacy by co-delivery of cytokines and temozolomide via ultrasound-gated redox-responsive extracellular vesicles. [Abstract]

2025 Dec 7;23(1):766. PMID: 41354801
Cell Discov

Cell type-specific NRBF2 orchestrates autophagic flux and adult hippocampal neurogenesis in chronic stress-induced depression. [Abstract]

2023 Aug 29;9(1):90. PMID: 37644025
Small

Unveiling the Influence of Tumor Microenvironment and Spatial Heterogeneity on Temozolomide Resistance in Glioblastoma Using an Advanced Human In Vitro Model of the Blood-Brain Barrier and Glioblastoma. [Abstract]

2023 Dec;19(52):e2302280. PMID: 37649234
Asian J Pharm Sci

Implantation of hydrogel-liposome nanoplatform inhibits glioblastoma relapse by inducing ferroptosis. [Abstract]

2023 May;18(3):100800. PMID: 37274924
Brain

Stepwise crosstalk between aberrant Nf1, Tp53 and Rb signalling pathways induces gliomagenesis in zebrafish. [Abstract]

2021 Mar 3;144(2):615-635. PMID: 33279959
J Control Release

NQO1-responsive Trimethyl lock benzoquinone: A cleavable linker strategy for antibody-drug conjugates. [Abstract]

2025 Dec 11:390:114534. PMID: 41389965
J Control Release

Heme Oxygenase-1 targeting exosomes for temozolomide resistant glioblastoma synergistic therapy. [Abstract]

2022 May;345:696-708. PMID: 35341901
MedComm (2020)

Integrated Multi-Omics Profiling to Characterize Molecular Subtypes and Reveal Potential Therapeutic Strategies for Colorectal Cancer. [Abstract]

2025 Dec 8;6(12):e70492. PMID: 41377767
Research (Wash D C)

Isovalerylspiramycin I Reprograms the Immunosuppressive and Temozolomide-Resistant Microenvironment by Inhibiting the Frizzled-5/Wnt/β-Catenin Pathway in Glioblastoma. [Abstract]

2025 Aug 13:8:0828. PMID: 40809457
MedComm

Sanggenon C inhibits cell proliferation and induces apoptosis by regulating the MIB1/DAPK1 axis in glioblastoma. [Abstract]

2023 Jun 19;4(4):e281. PMID: 37346933

Temozolomide purchased from MedChemExpress. Usage Cited in: MedComm. 2023 Jun 19;4(4):e281. [Abstract]

Temozolomide (TMZ) (300 μM) increases the expression of DAPK1, cleaved caspase-3 (C-Caspase3), and cleaved PARP (C-PARP) while decreasing MIB1 protein levels in both U-87 MG and LN-229 cells, and this effect is enhanced when combined with Sanggenon C (SC) (HY-N0617) (10 μM).
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Pharmacol Res

MUC1 promotes glioblastoma progression and TMZ resistance by stabilizing EGFRvIII. [Abstract]

2023 Jan:187:106606. PMID: 36516884
Cancer Lett

Aberrant PLAC8 expression characterizes glioblastoma with temozolomide resistance and an immunosuppressive microenvironment. [Abstract]

2025 May 19:625:217805. PMID: 40398706
Mol Psychiatry

Dual recombinase-mediated intersectional genetics defines the functional heterogeneity of neural stem cells in adult hippocampus. [Abstract]

2025 Aug;30(8):3516-3532. PMID: 39994425
Cancer Lett

High-content drug screening in zebrafish xenografts reveals high efficacy of dual MCL-1/BCL-XL inhibition against Ewing sarcoma. [Abstract]

2023 Feb 1:554:216028. PMID: 36462556
Cancer Lett

Fucoidan-coated nanoparticles target radiation-induced P-selectin to enhance chemoradiotherapy in murine colorectal cancer. [Abstract]

2021 Mar 1;500:208-219. PMID: 33232787
Int J Biol Sci

CD147 confers temozolomide resistance of glioma cells via the regulation of β-TrCP/Nrf2 pathway. [Abstract]

2021 Jul 13;17(12):3013-3023. PMID: 34421346
Acta Biomater

Virus-inspired nanocages potentiate glioblastoma sonochemotherapy via structure-function mimicry. [Abstract]

2025 Oct 15:S1742-7061(25)00770-6. PMID: 41106759
Cell Death Dis

Triggering of endoplasmic reticulum stress via ATF4-SPHK1 signaling promotes glioblastoma invasion and chemoresistance. [Abstract]

2024 Aug 1;15(8):552. PMID: 39090107
Acta Biomater

A Supramolecular Assembly Strategy for Hydrophilic Drug Delivery towards Synergistic Cancer Treatment. [Abstract]

2023 Jul 1:164:407-421. PMID: 37088157
Cell Death Dis

RNA binding protein NKAP protects glioblastoma cells from ferroptosis by promoting SLC7A11 mRNA splicing in an m6A-dependent manner. [Abstract]

2022 Jan 21;13(1):73. PMID: 35064112
Cell Death Dis

A positive feedback loop of lncRNA-RMRP/ZNRF3 axis and Wnt/β-catenin signaling regulates the progression and temozolomide resistance in glioma. [Abstract]

2021 Oct 16;12(11):952. PMID: 34657141
J Pharm Anal

A robust luminescent assay for screening alkyladenine DNA glycosylase inhibitors to overcome DNA repair and temozolomide drug resistance. [Abstract]

2023 May;13(5):514-522. PMID: 37305785

Temozolomide purchased from MedChemExpress. Usage Cited in: J Pharm Anal. 2023 May;13(5):514-522. [Abstract]

Temozolomide (TMZ; 10 μM; 24 h) enhances the Sunitinib-induced (3 μM; 24 h) expression of γ-H2Ax in T98G cells.

Temozolomide purchased from MedChemExpress. Usage Cited in: J Pharm Anal. 2023 May;13(5):514-522. [Abstract]

Temozolomide (TMZ; 10 μM; 24 h) enhances the Sunitinib-induced (3 μM; 24 h) expression of γ-H2Ax in T98G cells.
Int J Biol Macromol

Inhibition of replication factor C4-induced DNA damage repair reverses the chemoresistance of glioblastoma to temozolomide and reveals the synthetic lethal effect of combined targeting of checkpoint kinase 1. [Abstract]

2026 Mar:351:151067. PMID: 41747987
Int J Biol Macromol

TMEM165 promotes glioblastoma progression through epithelial-mesenchymal transition-mediated invasion and temozolomide chemoresistance. [Abstract]

2026 Jan;335(Pt 1):149216. PMID: 41308767
Int J Biol Macromol

Delactylation of H3K9 by Sirtuin6 inhibits MGMT transcription and reverses temozolomide resistance in glioblastoma. [Abstract]

2025 Sep 2;327(Pt 1):147332. PMID: 40907925
View

2023 Mar 13.
Acta Pharmacol Sin

Targeting PPARα activation sensitizes glioblastoma cells to temozolomide and reverses acquired resistance by inhibiting H3K18 lactylation. [Abstract]

2025 Jun 11. PMID: 40500345
Acta Pharmacol Sin

Pharmacologically inhibiting phosphoglycerate kinase 1 for glioma with NG52. [Abstract]

2021 Apr;42(4):633-640. PMID: 32737469
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Phytomedicine

Albanol B inhibits glioblastoma progression by inducing senescence and apoptosis via the RNF6/p27 signaling axis. [Abstract]

2025 Oct:146:157056. PMID: 40743902
Phytomedicine

Muscone restores anoikis sensitivity in TMZ-resistant glioblastoma cells by suppressing TOP2A via the EGFR/Integrin β1/FAK signaling pathway. [Abstract]

2024 May 5:129:155714. PMID: 38723526
EMBO Mol Med

Patient- and xenograft-derived organoids recapitulate pediatric brain tumor features and patient treatments. [Abstract]

2023 Dec 7;15(12):e18199. PMID: 38037472
Phytomedicine

Quercetin induces MGMT+ glioblastoma cells apoptosis via dual inhibition of Wnt3a/β-Catenin and Akt/NF-κB signaling pathways. [Abstract]

2023 Sep:118:154933. PMID: 37451151
Phytomedicine

Kaempferol inhibits non-homologous end joining repair via regulating Ku80 stability in glioma cancer. [Abstract]

2023 Jul 25:116:154876. PMID: 37210962
Phytomedicine

Xihuang Pill-destabilized CD133/EGFR/Akt/mTOR cascade reduces stemness enrichment of glioblastoma via the down-regulation of SOX2. [Abstract]

2023 Jun:114:154764. PMID: 36963368
ACS Appl Mater Interfaces

Overcoming the Blood-Brain Tumor Barrier with Docetaxel-Loaded Mesoporous Silica Nanoparticles for Treatment of Temozolomide-Resistant Glioblastoma. [Abstract]

2024 May 1;16(17):21722-21735. PMID: 38629735
Free Radic Biol Med

17β-estradiol induces temozolomide resistance through NRF2-mediated redox homeostasis in glioblastoma. [Abstract]

2021 Aug 20:172:430-440. PMID: 34186205
ACS Appl Mater Interfaces

Enhanced Efficacy of Temozolomide Loaded by a Tetrahedral Framework DNA Nanoparticle in the Therapy for Glioblastoma. [Abstract]

2019 Oct 30;11(43):39525-39533. PMID: 31601097
NPJ Precis Oncol

Refined high-content imaging-based phenotypic drug screening in zebrafish xenografts. [Abstract]

2023 May 18;7(1):44. PMID: 37202469
Neoplasia

Combining selinexor with alisertib to target the p53 pathway in neuroblastoma. [Abstract]

2022 Apr:26:100776. PMID: 35217309
Neoplasia

Tumor treating fields (TTFields) impairs aberrant glycolysis in glioblastoma as evaluated by [18F]DASA-23, a non-invasive probe of pyruvate kinase M2 (PKM2) expression. [Abstract]

2021 Jan;23(1):58-67. PMID: 33221711
Brain Behav Immun

Microglia-mediated neurogenesis is linked to cognitive deficits in a two-hit model of maternal immune activation and juvenile stress. [Abstract]

2025 Jun 25:129:649-661. PMID: 40578538
Brain Behav Immun

Pioglitazone alleviates maternal sleep deprivation-induced cognitive deficits in male rat offspring by enhancing microglia-mediated neurogenesis. [Abstract]

2020 Jul;87:568-578. PMID: 32032783
Biomed Pharmacother

A brain-penetrant CDK4/6 inhibitor - AU3-14 shows robust anti-tumor efficacy against glioblastoma. [Abstract]

2025 Aug:189:118340. PMID: 40651458
Biomed Pharmacother

Sitagliptin inhibits the survival, stemness and autophagy of glioma cells, and enhances temozolomide cytotoxicity. [Abstract]

2023 Jun:162:114555. PMID: 36966667
Oncogene

E3 ligase MAEA-mediated ubiquitination and degradation of PHD3 promotes glioblastoma progression. [Abstract]

2023 Apr;42(16):1308-1320. PMID: 36882523

Temozolomide purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Apr;42(16):1308-1320. [Abstract]

Temozolomide (TMZ; 60 mg/kg, i.g.; 5 consecutive days) treatment individually can suppress tumor growth, and the combination of knockdown MAEA and TMZ treatment can significantly inhibit tumor growth in mice (Fig A-B).
Cell Death Discov

Deciphering the STAT3-PXN positive feedback loop in GBM, IDH-wildtype: transcriptional regulation and inhibition of YB-1 ubiquitination. [Abstract]

2026 Mar 23;12(1):168. PMID: 41872167
Cell Rep

NAT10-dependent N4-acetylcytidine reprograms R-loops and promotes cancer stem cell growth. [Abstract]

2026 Jun 23;45(6):117408. PMID: 42228575
Neurotherapeutics

VP3.15, a dual GSK-3β/PDE7 inhibitor, reduces glioblastoma tumor growth though changes in the tumor microenvironment in a PTEN wild-type context. [Abstract]

2025 Mar 28:e00576. PMID: 40157890
Cell Rep

Targeting glioblastoma signaling and metabolism with a re-purposed brain-penetrant drug. [Abstract]

2021 Nov 2;37(5):109957. PMID: 34731610
Br J Cancer

Novel mutations of SRPX facilitate the stemness and malignant progression of glioma. [Abstract]

2025 Jul 15. PMID: 40665012
J Med Chem

Repurposing Linezolid in Conjunction with Histone Deacetylase Inhibitor Access in the Realm of Glioblastoma Therapies. [Abstract]

2025 Feb 13;68(3):2779-2803. PMID: 39836457
Oncogenesis

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Bioresorbable, electrospun nonwoven for delayed and prolonged release of temozolomide and nimorazole. [Abstract]

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Temozolomide purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2021 Feb 1:9:620883. [Abstract]

Analyses of Western blotting shows that Temozolomide (TMZ) treatment increases the expression of CD133, SOX2, OCT4, and NANOG, suggesting that TMZ treatment promotes glioma stem cells (GSCs) formation in GBM cells.
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Sci Rep

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2020 Sep 10;8(9):339. PMID: 32927743
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Temozolomide purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 17;7(20):29116-30. [Abstract]

U87MG glioma cells, and GBM8401 glioma cells are treated with DMSO or 20, 40, 60, or 80 μM of Hono, Mag or Hono-Mag combination for 24 hours. After treatment, the survival rate is analyzed using MTT tests. The right panels show Temozolomide (TMZ)-treated glioma cells which are regarded as a positive control.

Solvent & Solubility

In Vitro:

DMSO : 20.83 mg/mL (107.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2.86 mg/mL (14.73 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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, stored under nitrogen). 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

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

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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: 5 mg/mL (25.75 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[1]

The murine lymphoma cell line L5178Y of DBA/2 (H-2^d/H-2^d) origin is cultured in RPMI-1640 containing 10% fetal calf serum and antibiotics. Inhibition of PARP is obtained by treating cells (10⁵ cells/mL) with 8-hydroxy-2-methylquinazolin-4[³H]-1 (NU1025), at a concentration (25 μM) that abrogates PARP activity. Cells are then exposed to Temozolomide (7.5-125 μM) and are cultured for 3 days. Cell growth is evaluated by counting viable cells in quadruplicate, and apoptosis is assessed by flow cytometry analysis of DNA content. Long-term survival is analyzed by colony-formation assay^[1].

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

Animal Administration^[1]

Mice^[1]
Male B6D2F1 (C57BL/6×DBA/2) mice are used. L5178Y cells (10⁴ in 0.03 mL RPMI-1640) are then injected intracranially, through the center-middle area of the frontal bone to a 2-mm depth, using a 0.1-mL glass microsyringe and a 27-gauge disposable needle. To evaluate tumor cell growth, brains are fixed in 10% phosphate-buffered formaldehyde, and histologic sections (5 μm) are cut along the axial plane, stained with hematoxylin-eosin, and analyzed by light microscopy. Temozolomide is dissolved in DMSO (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. Because cytotoxicity induced by Temozolomide and PARP inhibitors can be improved by fractionated modality of treatment, in selected groups a total dose of 200 mg/kg Temozolomide is divided in 2 doses of 100 mg/kg given on days 2 and 3.

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

Purity & Documentation

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Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (645 KB)
- English - EN (645 KB)
- Français - FR (645 KB)
- Deutsch - DE (645 KB)
- Norwegian - NO (645 KB)
- Español - ES (645 KB)
- Swedish - SV (645 KB)
- Italian - IT (645 KB)
- Portuguese - PT (645 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tentori L, et al. Combined treatment with temozolomide and poly(ADP-ribose) polymerase inhibitor enhances survival of mice bearing hematologic malignancy at the central nervous system site. Blood. 2002 Mar 15;99(6):2241-4. [Content Brief]

[2]. Mathieu V, et al. Combining Anti-Human VEGF with temozolomide increases the antitumor efficacy of temozolomide in a human glioblastoma orthotopic xenograft model. Neoplasia. 2008 Dec;10(12):1383-92. [Content Brief]

[3]. Perazzoli G, et al. Temozolomide Resistance in Glioblastoma Cell Lines: Implication of MGMT, MMR, P-Glycoprotein and CD133 Expression. PLoS One. 2015 Oct 8;10(10):e0140131. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	5.1507 mL	25.7533 mL	51.5066 mL	128.7664 mL
	5 mM	1.0301 mL	5.1507 mL	10.3013 mL	25.7533 mL
	10 mM	0.5151 mL	2.5753 mL	5.1507 mL	12.8766 mL
DMSO	15 mM	0.3434 mL	1.7169 mL	3.4338 mL	8.5844 mL
	20 mM	0.2575 mL	1.2877 mL	2.5753 mL	6.4383 mL
	25 mM	0.2060 mL	1.0301 mL	2.0603 mL	5.1507 mL
	30 mM	0.1717 mL	0.8584 mL	1.7169 mL	4.2922 mL
	40 mM	0.1288 mL	0.6438 mL	1.2877 mL	3.2192 mL
	50 mM	0.1030 mL	0.5151 mL	1.0301 mL	2.5753 mL
	60 mM	0.0858 mL	0.4292 mL	0.8584 mL	2.1461 mL
	80 mM	0.0644 mL	0.3219 mL	0.6438 mL	1.6096 mL
	100 mM	0.0515 mL	0.2575 mL	0.5151 mL	1.2877 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.

Keywords

Temozolomide

193 Cited Publications

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Temozolomide

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

MCE Kinase Hinge Binder Fragment Library

Publications Citing Use of MedChemExpress (MCE) Temozolomide

Biological Activity

Chemical Information

Publications (193)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Temozolomide

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

MCE Kinase Hinge Binder Fragment Library

Publications Citing Use of MedChemExpress (MCE) Temozolomide

Biological Activity

Chemical Information

Publications (193)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Temozolomide Related Classifications

Cat. No.: HY-17364