2. Cell Cycle/DNA Damage
  3. DNA Alkylator/Crosslinker
  4. Trimelamol

Trimelamol  (Synonyms: CB 10-375; NSC 283162)

目录号: HY-106768
产品使用指南 技术支持

Trimelamol (CB10-375; NSC283162) 是一种高效的酸催化的 DNA 链间交联剂，由于其对血脑屏障的穿透性有限，神经毒性较低。Trimelamol 有抗肿瘤活性且克服铂类耐药性。Trimelamol 被用于对肺癌和卵巢癌的研究[1][2][3][4][5]。

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Trimelamol Chemical Structure

Trimelamol Chemical Structure

CAS No. : 64124-21-6

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Trimelamol 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Trimelamol (CB10-375; NSC283162) is a highly efficient acid-catalyzed DNA interstrand crosslinker with low neurotoxicity due to its limited BBB penetration. Trimelamol exhibits anti-tumor activity and overcomes platinum resistance. Trimelamol is investigated for lung and ovarian cancer research[1][2][3][4][5].

体外研究
(In Vitro)

Trimelamol 通过其 N-羟甲基基团直接发挥细胞毒性，移除药物后毒性不可逆。比 HMM 和 PMM 起效更快[1][2]。

Trimelamol (0.5-500 μM, 1 h) 交联是其主要抗肿瘤机制，在 32P-end-labelled pBR322 plasmid DNA 中，浓度 ≥ 2.5 μM 时显著交联DNA，酸性条件下交联效率更高[3]。

Trimelamol 具有广谱细胞毒性，且对铂耐药卵巢癌细胞有效 (IC50 范围: 8.5-55.4 μM)[4]。

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

Trimelamol 相关抗体:
体内研究
(In Vivo)

Trimelamol (15-60 mg/kg, i.p, 每日一次共五次持续四周) 在异种移植模型小鼠中对铂敏感/耐药卵巢癌，激素依赖性乳腺癌均有效，尤其在获得性耐药模型中表现突出[4]。

Trimelamol (7.5-60 mg/kg, i.p, 每日一次共五次持续三周) 通过肠胃外给药在在皮下移植T-61/ MX-1 肿瘤的 BALB/c 雌鼠中显著有效，在皮下移植 Br-10 肿瘤的 BALB/c 雌鼠中活性较弱。它在高剂量时表现出中度毒性，但在低浓度时毒性可控[5]。

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

Animal Model: (PXN/65, HX110, HX110P, HX62, T-61) xenograft tumor model in nude mice[4]
Dosage: 15 mg/kg, 30 mg/kg, 60 mg/kg for PXN/65, HX110, HX110P, HX62; 15 mg/kg for T-61
Administration: Intraperitoneal injection (i.p.), once a day for 5 days, 4 consecutive weeks
Result: had curative activity against PXN/65, HX110, HX110P, and T-61, but HX62 was non-curative but had a better T/C value (0.20) than cisplatin (0.40–0.84).
Animal Model: (T-61, MX-1, Br-10, R-27, MCF-7) xenograft tumor model in BALB/c famale mice(6-7 weeks, 20-22 g)[5]
Dosage: 60 mg/kg, 30 mg/kg, 15 mg/kg, 7.5 mg/kg for T-61, MX-1; 60 mg/kg for Br-10, R-27, MCF-7
Administration: Intraperitoneal injection (i.p.), once a day for 5 days, 3 consecutive weeks
Result: Completely regressed tumors in the T-61 model at 60 mg/kg. Significantly reduced tumor weight at 30 mg/kg (T/C = 3.8%).
Completely regressed tumors in the MX-1 model at both 60 and 30 mg/kg. Reduced tumor weight at 15 mg/kg (T/C = 8.3%).
Exhibited marginal activity in the Br-10 model at 60 mg/kg (T/C = 48.2%). Was insensitive in the R-27 and MCF-7 tumor models.
分子量

258.28

Formula

C9H18N6O3
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

Trimelamol 相关分类

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

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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.

Keywords:

Trimelamol64124-21-6CB 10-375 NSC 283162NSC283162NSC 283162NSC-283162DNA Alkylator/CrosslinkerBalb/CCancerNeurotoxicityWater soluble32P-end-labelled pBR322 plasmid DNAPC6 cellsPXN/65HX110Inhibitorinhibitorinhibit

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