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TMZ(Temozolomide) Alkylating Agent

Name: TMZ(Temozolomide)
Brand: Selleck Chemicals
SKU: S1237
Rating: 5 (246 reviews)

제품 번호S1237

Temozolomide (TMZ)는 DNA 고리의 질소 원자와 고리 외부 산소 그룹을 변형시킬 수 있는 단일 기능 SN-1 Alkylating Agent로, 화학적으로 MTIC로 전환되어 메틸디아조늄 양이온으로 분해되며, 이는 생리적 pH에서 DNA에 메틸 그룹을 전달합니다. 이는 L-1210 및 L-1210/BCNU 세포에서 DNA 손상 유도제입니다. 이 화합물은 apoptosis를 유도하고 항종양 활성을 나타냅니다.

TMZ(Temozolomide) DNA/RNA Synthesis 화학 Chemical Structure

화학 구조

분자량: 194.15

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품질 관리

배치: 순도: 99.99%

99.99

관련 타겟	HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF
기타 DNA/RNA Synthesis 억제제	CX-5461 (Pidnarulex) B02 SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Triapine (3-AP) Carmofur YK-4-279

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
Kelly	Growth Inhibition Assay		48 h		IC50=139.20 ± 5.95 μM	25960282
KellyCis83	Growth Inhibition Assay		48 h		IC50=251.00 ± 15.75 μM	25960282
SK-N-AS	Growth Inhibition Assay		48 h		IC50=227.70 ± 22.15 μM	25960282
SK-N-ASCis24	Growth Inhibition Assay		48 h		IC50=480.60 ± 101.15 μM	25960282
CHP-212	Growth Inhibition Assay		48 h		IC50=7.97 ± 0.69 μM	25960282
CHP-212Cis100	Growth Inhibition Assay		48 h		IC50=9.55 ± 0.88 μM	25960282
U87	Function Assay	100 μM	24-72 h		induces DcR1 expression	25808868
LN229	Growth Inhibition Assay	0-50 μM			IC50=16 μM	25750273
TR-LN229	Growth Inhibition Assay	0-50 μM			IC50=77 μM	25750273
U87	Apoptosis Assay	0–200 µM	24 h		enhances CQ induced apoptosis	25681668
U251MG	Apoptosis Assay	100 μM	48 h	PBS	induces apoptosis	25680464
U87MG	Apoptosis Assay	100 μM	48 h	PBS	induces apoptosis	25680464
U87	Growth Inhibition Assay	50-350 μM	48 h		inhibits cell growth slightly	25554223
U118	Growth Inhibition Assay	50-350 μM	48 h		inhibits cell growth slightly	25554223
U87	Function Assay	250/350 μM	48 h		enhances TMX-induced p-PKC-pan decrease	25554223
U118	Function Assay	250/350 μM	48 h		enhances TMX-induced p-PKC-pan decrease	25554223
U87	Growth Inhibition Assay	250/350 μM	48 h		increases the percentage of cells in S and G2/M cotreated with TMX	25554223
A375	Growth Inhibition Assay		48 h		IC50=265 μM	25524552
A2058	Growth Inhibition Assay		48 h		IC50=12 μM	25524552
M238	Growth Inhibition Assay		48 h		IC50=40 μM	25524552
M249	Growth Inhibition Assay		48 h		IC50=254 μM	25524552
M21	Growth Inhibition Assay		48 h		IC50=221 μM	25524552
U251	Cytotoxity Assay	20 μM	48 h		reduceds the percentages of colonies formed	25434381
LN229	Cytotoxity Assay	20 μM	48 h		reduceds the percentages of colonies formed	25434381
U373MG-LUC	Growth Inhibition Assay		72 h		IC50>600 μM	25431953
U87	Growth Inhibition Assay	25-200 μM	48 h		inhibits cell growth in a dose-dependent manner	25400745
U251	Growth Inhibition Assay	25-200 μM	48 h		inhibits cell growth in a dose-dependent manner	25400745
U251	Growth Inhibition Assay	100-400 μM	72/96 h		the anti-proliferative effect can be enhanced by gossypol enhanced	25375271
U373	Growth Inhibition Assay	100-400 μM	72/96 h		the anti-proliferative effect can be enhanced by gossypol enhanced	25375271
U343	Growth Inhibition Assay	100-400 μM	72/96 h		the anti-proliferative effect can be enhanced by gossypol enhanced	25375271
U87MG-luc2	Growth Inhibition Assay	100-400 μM	72/96 h		the anti-proliferative effect can be enhanced by gossypol enhanced	25375271
U87	Function Assay	200 μM	48 h		increases BRCC3 mRNA expression	25337721
U251	Function Assay	200 μM	48 h		increases BRCC3 mRNA expression	25337721
A172	Function Assay	200 μM	48 h		increases BRCC3 mRNA expression	25337721
U251	Function Assay	200 μM	48 h		increases the expression of BRCA1, BRCA2, RAD51 and FANCD2	25337721
A172	Function Assay	200 μM	48 h		increases the expression of BRCA1, BRCA2, RAD51 and FANCD2	25337721
U87	Function Assay	200 μM	24/72/120 h		increases γH2AX foci formation time-dependently	25337721
U251	Function Assay	200 μM	24/72/120 h		increases γH2AX foci formation time-dependently	25337721
A172	Function Assay	200 μM	24/72/120 h		increases γH2AX foci formation time-dependently	25337721
SNB19V	Growth Inhibition Assay		7 d	DMSO	GI50=35.7±12 μM	25277441
SNB19M	Growth Inhibition Assay		7 d	DMSO	GI50=469.9±88 μM	25277441
SNB19VR	Growth Inhibition Assay		7 d	DMSO	GI50=280.2±18 μM	25277441
U373V	Growth Inhibition Assay		7 d	DMSO	GI50=68.0±32 μM	25277441
U373M	Growth Inhibition Assay		7 d	DMSO	GI50=368.7±86 μM	25277441
U373VR	Growth Inhibition Assay		7 d	DMSO	GI50=288.8±33 μM	25277441
U87MG	Growth Inhibition Assay		7 d	DMSO	GI50=38.3±20 μM	25277441
HCT116	Growth Inhibition Assay		7 d	DMSO	GI50=579.9±32 μM	25277441
DLD1	Growth Inhibition Assay		7 d	DMSO	GI50=501.4±93 μM	25277441
MRC5	Growth Inhibition Assay		7 d	DMSO	GI50=449.4±8 μM	25277441
SNB19V	Function Assay	100 μM TMZ	0-72 h		increases γH2AX expression between 16 and 72 h	25277441
T98G	Growth Inhibition Assay	5/10/15 μM	24 h		induces cell death dose-dependently after concomitant-temozolomide with NPe6-PDT	25262961
U251	Growth Inhibition Assay	5/10/15 μM	24 h		induces cell death dose-dependently after concomitant-temozolomide with NPe6-PDT	25262961
T98G	Function Assay	15 μM	24 h		increases DNA-fragmentation in NPe6-PDT treated glioma cells	25262961
U251	Function Assay	15 μM	24 h		increases DNA-fragmentation in NPe6-PDT treated glioma cells	25262961
U-87 MG	Growth Inhibition Assay		72 h		IC50=0.93 mM	25245332
U-118 MG	Growth Inhibition Assay		72 h		IC50=1.05 mM	25245332
U87	Growth Inhibition Assay		24 h		IC50=260.34 μM	25173233
U87 GSLCs	Growth Inhibition Assay		24 h		IC50=766.11 μM	25173233
U87MG	Growth Inhibition Assay		72 h		IC50=15.625 μM	25050915
U251	Growth Inhibition Assay	100-400 μM	48 h	DMSO	inhibits cell growth in a dose-dependent manner	24623736
U87	Growth Inhibition Assay	100-400 μM	48 h	DMSO	inhibits cell growth in a dose-dependent manner	24623736
MDA-MB-231-br	Growth Inhibition Assay	0-10 μM	48 h	DMSO	inhibits cell growth in a dose-dependent manner	24623736
HCC-1937	Growth Inhibition Assay	0-300 μM	48 h	DMSO	inhibits cell growth in a dose-dependent manner	24623736
MDA-MB-231	Growth Inhibition Assay	0-40 μM	48 h	DMSO	inhibits cell growth in a dose-dependent manner	24623736
MDA-MB-468	Growth Inhibition Assay	0-500 μM	48 h	DMSO	inhibits cell growth in a dose-dependent manner	24623736
T47D	Growth Inhibition Assay	0-100 μM	48 h	DMSO	inhibits cell growth in a dose-dependent manner	24623736
MCF7	Growth Inhibition Assay	0-1000 μM	48 h	DMSO	inhibits cell growth in a dose-dependent manner	24623736
Hs683	Growth Inhibition Assay	0-1000 μM	96 h		IC50=128.9 μM	24495907
U87	Growth Inhibition Assay	0-1000 μM	96 h		IC50=18.45 μM	24495907
LNZ308	Growth Inhibition Assay	0-1000 μM	96 h		IC50=326.7 μM	24495907
U87	Apoptosis Assay	100 μM	48 h	DMSO	increases the caspase-3/7 activity	24481586
U251	Apoptosis Assay	100 μM	48 h	DMSO	increases the caspase-3/7 activity	24481586
U251	Growth Inhibition Assay		24 h		IC50=86.29 ± 1.58 μM	24326954
U251	Growth Inhibition Assay		48 h		IC50=75.34 ± 1.02 μM	24326954
U251	Growth Inhibition Assay		72 h		IC50=72.42 ± 1.45 μM	24326954
U251	Growth Inhibition Assay		96 h		IC50=69.82 ± 3.04 μM	24326954
T98G	Growth Inhibition Assay	0-750 μM	72/96 h		inhibits cell viability in a dose dependent manner	24324080
U251-MG	Growth Inhibition Assay	0-800 μM	72 h		inhibits cell viability in a dose dependent manner	24093630
D54-MG	Growth Inhibition Assay	0-800 μM	72 h		inhibits cell viability in a dose dependent manner	24093630
SHG-44	Growth Inhibition Assay	10-200 μM	96 h		IC50=9.73 ± 2.12 μM	24065569
U373	Growth Inhibition Assay	10-200 μM	96 h		IC50=10.13 ± 1.02 μM	24065569
HT-29	Function Assay	500 μM	24/48 h		enhances the levels of γ-H2AX	24038068
PC-3	Growth Inhibition Assay	0-25 μM	48 h		inhibits cell growth which can be potentiated by lycopene	23746934
PC-3	Apoptosis Assay	25 μM	48 h		induces apoptosis which can be potentiated by lycopene	23746934
T98G	Growth Inhibition Assay	50-400 μM	144 h		inhibits cell viability in a dose dependent manner	23715499
U87-MG	Growth Inhibition Assay	100 µM	72 h		inhibits cell growth which can be enhanced by GTB	23696788
U251-MG	Growth Inhibition Assay	100 µM	72 h		inhibits cell growth which can be enhanced by GTB	23696788
LNT-229	Growth Inhibition Assay	3-100 μM	24 h		inhibits clonogenic survival in a dose-dependent manner	23667632
T98G	Growth Inhibition Assay	10-700 μM	24 h		inhibits clonogenic survival in a dose-dependent manner	23667632
U87	Function Assay	100 µM	3 h		elevates the levels of pChk1 and pChk2	23667469
HCT116	Function Assay	100 µM	3 h		induces the Chk1 Phosphorylation	23667469
HCT3-6	Function Assay	100 µM	3 h		induces the Chk1 Phosphorylation	23667469
U-87	Growth Inhibition Assay	0-40 μM	12 d		inhibits cell growth in a dose-dependent manner	23645729
U-87	Apoptosis Assay	0-40 μM	3/6 d		induces apoptosis in both dose- and time-dependent manner	23645729
U-87	Function Assay	0-40 μM	3/6 d		induces autophagy in both dose- and time-dependent manner	23645729
GB-SCC010	Growth Inhibition Assay		4 d		IC50=226 μM	23612755
GB-SCC026	Growth Inhibition Assay		4 d		IC50=53.1 μM	23612755
GB-SCC028	Growth Inhibition Assay		4 d		IC50=167 μM	23612755
U87	Growth Inhibition Assay		4 d		IC50=45.2 μM	23612755
U87 stem cell	Growth Inhibition Assay		4 d		IC50=66.7 μM	23612755
TLX5 lymphoma	Cytotoxicity assay				IC50 = 5 μM	7739008
GM892 A	Cytotoxicity assay				IC50 = 7.6 μM	7739008
TLX5 lymphoma	Cytotoxicity assay				IC50 = 5 μM	12459014
HCT116	Cytotoxicity assay		4 days		IC50 = 4.34 μM	19800803
SNB75	Antiproliferative assay	10 uM	24 hrs		Antiproliferative activity against human SNB75 cells at 10 uM after 24 hrs by SRB assay	22268526
C6	Antiproliferative assay	100 uM	48 hrs		Antiproliferative activity against rat C6 cells at 100 uM after 48 hrs by neutral red incorporation assay	22268526
SF295	Antiproliferative assay	10 uM	24 hrs		Antiproliferative activity against human SF295 cells at 10 uM after 24 hrs by SRB assay	22268526
U87	Antiproliferative assay		5 days		IC50 = 49 μM	22608389
U138MG	Cytotoxicity assay		48 hrs		IC50 = 26 μM	23069682
C6	Cytotoxicity assay		48 hrs		IC50 = 34 μM	23069682
A2780	Antitumor assay		5 days		IC50 = 8.5 μM	23895620
A2058	Antitumor assay		5 days		IC50 = 35.5 μM	23895620
SNB19	Antitumor assay		5 days		IC50 = 37 μM	23895620
M8	Apoptosis assay	50 to 100 uM	48 hrs		Induction of apoptosis in human M8 cells assessed as apoptotic/necrotic cells at 50 to 100 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis	24125877
SK-MEL-30	Apoptosis assay	100 uM	48 hrs		Induction of apoptosis in human SK-MEL-30 cells assessed as apoptotic/necrotic cells at 100 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis relative to control	24125877
SK-MEL-30	Apoptosis assay	50 uM	48 hrs		Induction of apoptosis in human SK-MEL-30 cells assessed as apoptotic/necrotic cells at 50 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis relative to control	24125877
MNT1	Apoptosis assay	100 uM	48 hrs		Induction of apoptosis in human MNT1 cells assessed as apoptotic/necrotic cells at 100 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis relative to control	24125877
MNT1	Apoptosis assay	50 uM	48 hrs		Induction of apoptosis in human MNT1 cells assessed as apoptotic/necrotic cells at 50 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis relative to control	24125877
A2780	Cytotoxicity assay		5 days		Cytotoxicity against human A2780 cells after 5 days by MTT assay	24900418
A2780/CP70	Cytotoxicity assay		5 days		Cytotoxicity against MMR-deficient human A2780/CP70 cells after 5 days by MTT assay	24900418
GBM 047T	Antitumor assay	20 uM	1 to 2 weeks		Tumoricidal effect in patient derived GBM 047T cells assessed as reduction in neurosphere formation at 20 uM after 1 to 2 weeks by 3D tumor clonogenic assay	26355532
GBM 464T	Antitumor assay	20 uM	1 to 2 weeks		Tumoricidal effect in patient derived GBM 464T cells assessed as reduction in neurosphere formation at 20 uM after 1 to 2 weeks by 3D tumor clonogenic assay	26355532
U87MG	Function assay		3 hrs		Induction of DNA alkylation in human U87MG cells assessed as increase in N7-MedG formation after 3 hrs by LC-MS/MS analysis	27614414
U87MG	Antitumor assay				Antitumor activity against human U87MG cells orthotopically xenografted in Harlan nude mouse brain assessed as induction of slow tumor growth at 50 umol/kg, iv administered once daily for 5 days	27614414
U87MG	Antitumor assay				Antitumor activity against human U87MG cells orthotopically xenografted in Harlan nude mouse brain assessed as increase in mouse survival at 50 umol/kg, iv administered once daily for 5 days	27614414
MDCK	Cytotoxicity assay		24 hrs		Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability incubated for 24 hrs measured after 7 days under normoxic condition by methylene blue staining based clonogenic survival assay	27823879
MDCK	Cytotoxicity assay		24 hrs		Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability incubated for 24 hrs measured after 7 days under hypoxic condition by methylene blue staining based clonogenic survival assay	27823879
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
C6	Cytotoxicity assay		4 days		EC50 = 16.5 μM	ChEMBL
U87	Cytotoxicity assay		72 hrs		IC50 = 19.38 μM	ChEMBL
SNB19	Growth inhibition assay		7 days		GI50 = 35.7 μM	ChEMBL
SNB19	Growth inhibition assay		7 days		GI50 = 45.6 μM	ChEMBL
U373	Function assay	100 uM	72 hrs		Induction of double stranded DNA break in empty vector transfected human U373 cells assessed as increase in gamma-H2AX level at 100 uM after 72 hrs by flow cytometry	ChEMBL
Glioma	Antitumor assay				Antitumor activity against Homo sapiens (human) Glioma cells xenografted in transgenic mouse assessed as mouse survival	ChEMBL
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	194.15	화학식	C₆H₆N₆O₂	보관 (수령일로부터)	3 years-20°C （in the dark）powder
CAS 번호	85622-93-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	NSC 362856,CCRG 81045,Methazolastone			Smiles	CN1C(=O)N2C=NC(=C2N=N1)C(=O)N

용해도

In vitro
배치:

DMSO : 39 mg/mL (200.87 mM) 50°C 수조에서 가온; 초음파 처리;
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 10 mg/mL (超声加热五分钟)

Ethanol : Insoluble

DMSO : 39 mg/mL (200.87 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 39 mg/mL (200.87 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 5 mg/mL

Ethanol : Insoluble

DMSO : 19 mg/mL (97.86 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 3 mg/mL

Ethanol : Insoluble

DMSO : 20 mg/mL (103.01 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 2.5 mg/mL

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 30%PEG300 2 65%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.000mg/ml (10.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 650 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.000mg/ml (10.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	0.400mg/ml (2.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.000mg/ml (10.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	5.000mg/ml (25.75mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

특징	Methazolastone is a second-generation alkylating agent.
Targets/IC₅₀/Ki	DNA replication (L-1210, L-1210/BCNU cells)
시험관 내(In vitro)	Temozolomide (TMZ)는 L-1210 및 L-1210/BCNU 세포주에서 유사한 양으로 존재하고 유사한 속도로 복구되는 DNA 알칼리-불안정 부위의 형성을 유발합니다. L-1210에서는 나타나지만 L-1210/BCNU에서는 나타나지 않는 이 화합물은 SL-G2-M 단계에서 세포의 정지를 유도합니다. 화학요법에 민감한 세포와 내성 세포 (D54-R 및 U87-R) 모두의 민감도는 고산소증 하에서 유의하게 향상됩니다. TMZ와 고산소증 모두 ERK p44/42 MAPK (Erk1/2)의 인산화 증가와 관련이 있지만, D54-R 세포에서는 정도가 약하며, 이는 Erk1/2 활성이 고산소증 및 TMZ-매개 세포 사멸 조절에 관여할 수 있음을 시사합니다. 고산소증은 MAPK 관련 경로를 통해 Apoptosis 유도를 통해 GBM 세포에서 독성을 강화합니다. 단핵구에서 DNA 손상 반응 경로인 ATM-Chk2 및 ATR-Chk1을 유도하여 p53 활성화를 초래합니다. 이 화합물에 대한 만성 노출은 후천적 TMZ-내성을 유발하고 miR-21 발현을 증가시킵니다. 이 화합물로 치료하면 GADD153 및 GRP78 단백질 발현 증가와 프로카스파제 12 단백질 감소와 함께 소포체 (ER) 스트레스를 유발합니다. 미토콘드리아 손상 및 ER 스트레스 의존적 메커니즘을 통해 Autophagy를 유도하여 교모세포종 세포를 보호합니다.
생체 내(In vivo)	종양 이식 후 1-5일 동안 5일 연속으로 매일 40 mg/kg의 i.p. 용량을 투여한 후, TMZ(Temozolomide)는 L-1210에서 수명을 86%, L-1210/BCNU에서 22% 증가시킵니다. L-1210/BCNU에서는 100 μM 또는 200 μM 치료 후 효과가 나타나지 않았습니다. 이 화합물 400 μM만이 전사 분열기 세포의 축적을 유도했지만, L-1210보다 훨씬 적었습니다. L-1210/BCNU에서 SL-G2-M 단계 세포의 최대 축적은 48-72시간 후 처리되지 않은 세포의 23%에 비해 약 30%였습니다. L-1210 백혈병을 앓는 쥐에게 i.v.로 이 화합물(40 mg/kg)을 투여했을 때도 SL-G2-M 단계 세포의 축적이 발생했습니다. 동일한 약물 용량을 투여한 쥐의 L-1210/BCNU 세포에서는 이러한 효과가 나타나지 않았습니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/3621181/ [2] https://pubmed.ncbi.nlm.nih.gov/22763762/ [3] https://pubmed.ncbi.nlm.nih.gov/22768182/ [4] https://pubmed.ncbi.nlm.nih.gov/22753745/ [5] https://pubmed.ncbi.nlm.nih.gov/22745676/ [6] https://pubmed.ncbi.nlm.nih.gov/22627392/

적용 분야

방법	바이오마커	PMID
Western blot	pERK / ERK / p-p38 / p38 DR5 / c-FLIP / Survivin / XIAP	24436439
Growth inhibition assay	Cell viability	25751281
Immunofluorescence	Phalloidin / Phospho-H2A.X cleaved caspase-3	27375225

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT05128734	Not yet recruiting	Breast Cancer Triple Negative	AHS Cancer Control Alberta	July 1 2024	Phase 2
NCT06161974	Not yet recruiting	High Grade Glioma\|Astrocytoma\|Astrocytoma Grade III\|Astrocytoma Grade IV\|Diffuse Intrinsic Pontine Glioma\|WHO Grade III Glioma\|WHO Grade IV Glioma\|Metastatic Brain Tumor\|Diffuse Midline Glioma H3 K27M-Mutant\|Thalamus Tumor\|Spinal Tumor\|IDH1 Mutation\|IDH1 R132\|IDH1 R132C\|IDH1 R132H\|IDH1 R132S\|IDH1 R132G\|IDH1 R132L\|Oligodendroglioma	Rigel Pharmaceuticals\|Nationwide Children''s Hospital	June 2024	Phase 2
NCT04967690	Not yet recruiting	Newly Diagnosed Glioblastoma	Double Bond Pharmaceutical AB	January 2024	Phase 1
NCT05698524	Recruiting	Recurrent High Grade Glioma\|Anaplastic Astrocytoma\|Anaplastic Oligodendroglioma\|Glioblastoma\|Gliosarcoma	University of Nebraska\|Xynomic Pharmaceuticals Inc.	June 26 2023	Phase 1
NCT04945148	Not yet recruiting	Glioblastoma IDH-wildtype	Hopital Foch\|National Cancer Institute France	May 2023	Phase 2

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