1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis DNA Alkylator/Crosslinker
  3. Cystemustine

Cystemustine 是一种 DNA 抑制剂,Cystemustine 能造成 DNA 交联,从而抑制肿瘤细胞增值。Cystemustine 也能通过干扰细胞周期、诱导细胞再分化以及改变磷脂代谢等方式发挥其细胞毒性作用。Cystemustine 在小鼠体内具有较高的抗肿瘤活性和较短的血浆半衰期,受昼夜给药时间的影响。Cystemustine 可被用于多种恶性肿瘤研究,包括黑色素瘤、胶质瘤、肾癌、头颈癌和结直肠癌等 。

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Cystemustine Chemical Structure

Cystemustine Chemical Structure

CAS No. : 79955-36-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cystemustine is a DNA inhibitor (a chloroethyl nitrosourea, CENU). Cystemustine can cause DNA cross-linking, thereby inhibiting the proliferation of tumor cells. Cystemustine can also exert cytotoxic effects by interfering with the cell cycle, inducing cell re-differentiation, and altering phospholipid metabolism. Cystemustine exhibits high anti-tumor activity and a relatively short plasma half-life in mice. Cystemustine can be used for the study of various malignant tumors, including melanoma, glioma, renal cancer, head and neck cancer, and colorectal cancer, etc[1][2][3][4][5][6].

体外研究
(In Vitro)

Cystemustine (100, 200 μM, 2 h) 单独使用时不会造成 DNA 损伤,但是与 O6-苄基-N2-乙酰鸟苷 (BNAG) 连用时可显著增加 M3Dau 细胞 DNA 损伤数量[3]
Cystemustine (50 μM, 4 h) 在 M4Beu 细胞中造成细胞毒性,但当与 lGgBZ (一种 O6-alkylguanine-DNA alkyltransferase 抑制剂) 连用时效果增强[6]

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

RT-PCR[3]

Cell Line: M3Dau cells
Concentration: 100, 200 μM or with BNAG (300 μM)
Incubation Time: 2 h or after 4 h
Result: Did not significantly modify the level of amplification of the DNA fragment alone.
Cause 1.85 or 2.55 injuries respectively with combined with BNAG.
体内研究
(In Vivo)

Cystemustine (35 mg/kg, i.v., 单次给药,持续 55 天) 存在大振幅昼夜戒律变化规律,最低毒性为光照开始后 15-19 小时,最高毒性为光照开始后 7 小时[2]
Cystemustine (15 mg/kg, i.v. or 直接注射到肿瘤内,第 1-19 天给药) 在小鼠黑色素瘤模型中诱导了细胞形态、细胞周期和黑色素含量变化[4]
Cystemustine (15 mg/kg, 直接注射到肿瘤内, 第 11-18 天给药)使黑色素瘤肿瘤在小鼠模型中呈现出一种新的磷脂代谢表型[5]

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

Animal Model: Active span of the rest-activity circadian cycle in male B6DZFI mice (9-10 weeks)[2]
Dosage: 35 mg/kg
Administration: Intravenous injection (i.v.), single dose for 55 days
Result: Survival rate ranged from only 3.8% at HALO up to 87.5 and 88.2% at 15 and 19 HALO, respectively.
Weight loss ranged from -16.6% at 15 HALO to -27.3% at 3 HALO.
Animal Model: Melanoma model established in male C57BL6/6J mice, 6-8 weeks[4]
Dosage: 15 mg/kg
Administration: Intravenous injection (i.v.) or injected directly into the tumor (i.t.), at days 1, 5, and 9 after B16 cell inoculation or at days 11, 14, and 19 after inoculation
Result: Exhibited alteration in cell morphology and increase in melanin content.
Strongly reduced the number of mitoses/microscopic field by 10-fold.
Animal Model: Melanoma model established in male C57BL6/6J mice, 6-8 weeks[5]
Dosage: 15 mg/kg
Administration: Injected directly into the tumor (i.t.), at days 11, 14, and 18 from B16 cell inoculation
Result: Induced a sustained redifferentiation pattern.
Exhibited transient increase in Cho, GPC, and GPE and sustained elevation of PC and PE during growth inhibition.
Exhibited sustained overexpression of PC and PE during growth recovery.
分子量

257.70

Formula

C6H12ClN3O4S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Cystemustine
目录号:
HY-106435
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