1. Apoptosis
  2. Thymidylate Synthase
  3. Idetrexed

Idetrexed  (Synonyms: BGC 945; ONX-0801; CB 300945)

目录号: HY-10822
产品使用指南 技术支持

Idetrexed (ONX 0801) 是一种胸苷酸合酶 (thymidylate synthase (TS)) 抑制剂,Ki 值为 1.2 nM。Idetrexed 可特异性转运至 α-叶酸受体 (α-FR) 过表达的肿瘤,例如卵巢癌。

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Idetrexed

Idetrexed Chemical Structure

CAS No. : 501332-69-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Idetrexed (ONX 0801) is a thymidylate synthase (TS) inhibitor with a Ki of 1.2 nM. Idetrexed can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer[1][2].

体外研究
(In Vitro)

Idetrexed (BGC 945) 旨在通过更有效地靶向过度表达 α-FR[1] 的癌细胞来进一步降低毒性。
Idetrexed (BGC 945) 在 A431、A431-FBP、KB、IGROV-1 和 JEG-3 细胞中的 IC50 值分别为 6.6 μM、1.1 nM、3.3 nM、90 nM 和 0.32 μM[2]

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

体内研究
(In Vivo)

Idetrexed (BGC 945) (100 mg/kg,腹腔/静脉注射) 在肿瘤中的半衰期 (28 小时) 比其他组织更长[2]
Idetrexed (BGC 945) (100 mg/kg,每日一次, 16 天) 不会导致体重减轻、主要器官的宏观毒性症状或肾功能改变[2]
Idetrexed (BGC 945) 100 mg/kg 剂量在 4-72 小时内可诱导肿瘤 dUrd 增加 5-20 倍,且血浆浓度不升高,这与肿瘤靶向性一致[2]

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

Animal Model: Mice (on the folate-free diet for 5 days were transplanted with tumor and the implants)[2].
Dosage: 100 mg/kg (Pharmacokinetic Analysis).
Administration: Single i.p. or iv injection.
Result: After i.p. injection, the compound was well absorbed from the peritoneal cavity. The plasma AUC was 50% higher for i.p. compared with i.v. administration and was also higher in spleen, kidney, and liver by this route. Tumor AUC was similar via either route.
Clinical Trial
分子量

647.63

Formula

C32H33N5O10

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
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