货号:A137834
同义名:
NSC 362856; CCRG 81045
Temozolomide是一种DNA甲基化剂和烷基化细胞毒药物,广泛用于治疗脑癌、星形胶质瘤和胶质母细胞瘤。它能够诱导细胞凋亡,具有抗肿瘤和抗血管生成作用。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
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产品名称 | DNA synthesis ↓ ↑ | helicase ↓ ↑ | RdRp ↓ ↑ | ribonucleotide reductase ↓ ↑ | tRNA synthetase ↓ ↑ | YB-1 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Fexinidazole | ✔ | 98% | |||||||||||||||||
Daptomycin | ✔ | 98% | |||||||||||||||||
Blasticidin S·HCl | ✔ | 98% | |||||||||||||||||
Metronidazole | ✔ | 98% | |||||||||||||||||
Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
Triglycidyl isocyanurate | ✔ | p53 | 98+% | ||||||||||||||||
Nedaplatin | ✔ | 99%+ | |||||||||||||||||
Oxolinic acid | ✔ | 98+% | |||||||||||||||||
Bendamustine | ✔ | 98+% | |||||||||||||||||
Trifluridine | ✔ | 98% | |||||||||||||||||
Robinetin | ✔ | 99%+ | |||||||||||||||||
Carboplatin | ✔ | 99% | |||||||||||||||||
Cidofovir | ✔ | 99% | |||||||||||||||||
Cisplatin | ✔ | 99% | |||||||||||||||||
Cytarabine |
++++
DNA synthesis, IC50: 16 nM |
98% | |||||||||||||||||
Acelarin |
++++
DNA synthesis, EC50: 0.2 nM |
99%+ | |||||||||||||||||
Oxaliplatin | ✔ | 98% | |||||||||||||||||
YK-4-279 | ✔ | 99%+ | |||||||||||||||||
ML216 |
+
BLM636-1298, IC50: 0.97 μM BLMfull-length, IC50: 2.98 μM |
99%+ | |||||||||||||||||
RK-33 | ✔ | 98% | |||||||||||||||||
Brr2-IN-3 | ✔ | 99%+ | |||||||||||||||||
Phen-DC3 Trifluoromethanesulfonate | ✔ | 95% | |||||||||||||||||
Favipiravir | ✔ | 99% | |||||||||||||||||
Suramin sodium salt |
++
RdRp, IC50: 0.26 μM |
99%+ | |||||||||||||||||
Clofarabine |
++
Ribonucleotide reductase, IC50: 65 nM |
97% | |||||||||||||||||
Didox | ✔ | 98% | |||||||||||||||||
(E)-3-AP | ✔ | 99% | |||||||||||||||||
Halofuginone |
+++
prolyl-tRNA synthetase, Ki: 18.3nM |
99%+ | |||||||||||||||||
BC-LI-0186 |
+++
Leucyl-tRNA synthetase, Kd: 42.1 nM Leucyl-tRNA synthetase, IC50: 46.11 nM |
98% | |||||||||||||||||
SU056 |
+
YB-1, IC50: 1.73 μM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | DNA damage is an abnormal chemical structure in DNA, while a mutation is a change in the sequence of standard base pairs. DNA damages cause changes in the structure of the genetic material and prevent the replication mechanism from functioning and performing properly. Temozolomide is converted to the active metabolite 5-(3-methyltriazen-1-yl) imidazole-4-carboxamide (MTIC) by non-enzymatic chemical conversion that produces DNA damage[3]. In vitro, temozolomide exhibited anti-proliferation to human malignant glioma cell lines U373MG, U87MG, and T98G with IC50 values of 40, 30 and 350 μM, respectively. Temozolomide induced apoptosis in the MGMT expressing cells occurred through AKT-Glycogen-Synthase-Kinase-3β signaling and is mediated by myelocytomatosis oncoprotein[4]. Temozolomide treatment at concentration of 100 mM for 72h increased the population at the G2/M phase and decreased the population at the G1 phase in all malignant glioma cells. In addition, temozolomide induced autophagy in U373-MG cells[5]. In vivo, administration of 40 mg/kg temozolomide significantly increased survival times in a B16F10 mouse metastatic melanoma model[6]. Treatment with temozolomide at dose of 2.5 mg/kg daily for 4 weeks resulted in a 78.30% tumor suppression, and reduced microvessel density in the glioblastoma orthotopic xenograft model[7]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
A172 | 200 μM | Function Assay | 48 h | increases BRCC3 mRNA expression | 25337721 |
A172 | 200 μM | Function Assay | 48 h | increases the expression of BRCA1, BRCA2, RAD51 and FANCD2 | 25337721 |
A172 | 200 μM | Function Assay | 24/72/120 h | increases γH2AX foci formation time-dependently | 25337721 |
A2058 | Growth Inhibition Assay | 48 h | IC50=12 μM | 25524552 | |
Dose | Nude Mice: 0.9 mg/kg - 266 mg/kg[1] (p.o.) Mice: 50 mg/kg[2] (i.v.) | ||||||||||
Administration | p.o., i.v. | ||||||||||
Pharmacokinetics |
|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00611247 | Leukemia, Myeloid | Phase 2 | Completed | - | United States, California ... 展开 >> Stanford University School of Medicine Stanford, California, United States, 94305 收起 << |
NCT00611247 | - | Completed | - | - | |
NCT00869050 | Neuroendocrine Tumors | Phase 2 | Completed | - | United States, New York ... 展开 >> Columbia University Medical Center New York, New York, United States, 10032 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
5.15mL 1.03mL 0.52mL |
25.75mL 5.15mL 2.58mL |
51.51mL 10.30mL 5.15mL |
CAS号 | 85622-93-1 |
分子式 | C6H6N6O2 |
分子量 | 194.15 |
SMILES Code | C1=NC(=C2[N]1C(N(C)N=N2)=O)C(N)=O |
MDL No. | MFCD00866492 |
别名 | NSC 362856; CCRG 81045; MB 39831; TMZ |
运输 | 蓝冰 |
InChI Key | BPEGJWRSRHCHSN-UHFFFAOYSA-N |
Pubchem ID | 5394 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 20 mg/mL(103.01 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 2.5 mg/mL(12.88 mM),配合低频超声助溶 |
动物实验配方 |
5% DMSO+30% PEG 300+water 2 mg/mL |