| CAS |
No.52-24-4 |
| 中文名称 |
塞替派 |
| 英文名称 |
Thio-TEPA |
| 别名 |
三亚乙基硫代磷酰胺;Tiofosfamid;Tiofosyl;Triethylenethiophosphoramide; |
| 分子式 |
C6H12N3PS |
| 分子量 |
189.22 |
| 溶解性 |
Soluble in DMSO ≥4mg/mL(Need ultrasonic) |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 |
冷藏运输 |
| MDL |
MFCD00145452 |
| SMILES |
C1CN1P(=S)(N2CC2)N3CC3 |
| InChIKey |
FOCVUCIESVLUNU-UHFFFAOYSA-N |
| InChI |
InChI=1S/C6H12N3PS/c11-10(7-1-2-7，8-3-4-8)9-5-6-9/h1-6H2 |
| PubChem CID |
5453 |
| 靶点 |
DNA Alkylator |
| 通路 |
DNA Damage/DNA Repair |
| 背景说明 |
Thio-TEPA 是一种 DNA 烷化剂 (DNA alkylator)，具有抗肿瘤活性。 |
| 生物活性 |
Thio-TEPA is a DNA alkylating agent， with antitumor activity.[1-2] |
| In Vitro |
Thio-TEPA 在大鼠肝切片孵育中表现出烷化活性。Thio-TEPA 不影响大鼠肝切片的活力，并且在 2、5、10 mM 的所有剂量下都不会在切片中积累[1]。 |
| In Vivo |
Thio-TEPA (20 mg/kg，ip) 与全身照射 (TBI) 在前 10 周内增强了供体型血液嵌合体，但并不显著高于单独的 TBI 组。Thio-TEPA 单独改善小鼠的短期和长期植入[2]。 |
| 细胞实验 |
The effect of Thio-TEPA on slice viability is studied by the determination of intracellular potassium (K+) leakage. Intracellular K+ is measured by flame photometry and is expressed in relation to the DNA content as measured using fluorometry. Thio-TEPA is added at concentrations of 1， 2， 5， and 10 mM and slices are incubated for 6， 12， and 24 h. The results are compared with the values found for drug-free controls. Thio-TEPA in medium and slices is measured following 3， 6， and 9 h incubation at the three highest concentrations. Krebs-HEPES buffer is used as the slicing buffer and Waymouth‘s MB 752/1 medium supplemented with 10 μg gentamycin is used as the incubation medium[1]. |
| 动物实验 |
Mice[2]Male C57BL/6JIco mice， 19 weeks old， 25 to 30 g， are used as recipients. Congenic C57BL/6J-Gpi-1a/Gpi-1a (B6-Gpi-1a) and BALB.B10LiLa (Gpi-1a) mice are used as a source of syngeneic and allogeneic donor bone marrow， respectively. The latter combination is H-2-compatible (both H-2b)， but mismatched on a number of minor histocompatibility loci. Thio-TEPA is dissolved in PBS and injected i.p. at a single bolus of 20 mg/kg. Preliminary pilot experiments have established that this approximated to the maximal tolerated dose when higher doses result in lethal gastrointestinal toxicity. Cyclophosphamide (CY) is dissolved in PBS and administered i.p. at a single dose of 200 mg/kg. Total body irradiation is delivered using a 137Cs γ-irradiation unit at a dose rate of 87 cGy/min to a dose of 5 Gy. After Thio-TEPA treatment the mice are maintained on neomycin (3.5 g/L sterile drinking water) for 2 weeks to minimize the possible problems of endotoxemia via gut toxicity[2]. |
| 数据来源文献 |
[1]. Hagen B， et al. Metabolism and alkylating activity of thio-TEPA in rat liver slice incubation. Cancer Chemother Pharmacol. 1991;28(6):441-7.
[2]. Down JD， et al. Thiotepa improves allogeneic bone marrow engraftment without enhancing stem cell depletion in irradiated mice. Bone Marrow Transplant. 1998 Feb;21(4):327-30. |
| 规格 |
5mg 10mg 25mg 50mg 100mg |
| 单位 |
瓶 |
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英语
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