2. Metabolic Enzyme/Protease
  3. 17β-HSD
  4. Odafosfamide

Odafosfamide  (Synonyms: (S)-OBI-3424; (S)-TH-3424; AST-3424)

目录号: HY-149040
产品使用指南 技术支持

Odafosfamide ((S)-OBI-3424) 是一种高选择性的由醛酮还原酶 1C3 (AKR1C3() 激活的前体药物双烷化剂。Odafosfamide 对 AKR1C3 表达高的细胞系具有有效的细胞毒性。Odafosfamide 在多种高表达 AKR1C3 的肿瘤 (如肝癌、非小细胞肺癌、白血病) 中表现出抗肿瘤活性。Odafosfamide 可用于癌症研究。

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Odafosfamide

Odafosfamide Chemical Structure

CAS No. : 2097713-69-2

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Odafosfamide 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

Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research[1][2].

体外研究
(In Vitro)

Odafosfamide (72-96 小时) 对 AKR1C3 蛋白和 RNA 表达水平较高的肝癌细胞 (SNU-475，SNU-449，C3A 显示出细胞毒性，IC50 分别为 15 nM，45 nM，5 nM) 和非小细胞肺癌细胞 (NSCLC) (NCI-H1944，NCI-H2228，NCIH1755，NCI-H1563，NCI-H2110，NCI-H1792，IC50 分别为 2.3 nM，0.21 nM，8.2 nM，2.5 nM，1.1 nM，4.5 nM)[1]。

Odafosfamide 对 19 种代表 B-ALL、T-ALL 和 ETP-ALL 的白血病细胞系显示出潜在的抗白血病活性 (IC50 分别为 60.3 nM/L、9.7 nM/L、31.5 nM/L)[2]。

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

Odafosfamide 相关抗体:
体内研究
(In Vivo)

Odafosfamide (1.25-5 mg/kg，静脉注射，每周一次，共 2 周) 可抑制 HepG2 原位异种移植小鼠模型中的肿瘤生长[1]。

Odafosfamide (0.625-1.25 mg/kg，静脉注射，每周一次，共 2 个周期；停药一周，再进行 2 个周期，每周一次) 可抑制 H460 皮下移植小鼠模型中的肿瘤生长[1]。

Odafosfamide (2.5 mg/kg, 5 mg/kg，静脉注射，每周一次，共 4-5 次) 可抑制 (CRPC) VCaP, SNU-16 和 A498 异种移植小鼠模型中的肿瘤生长[1]。

Odafosfamide (1.25-5 mg/kg，静脉注射，每周一次，共 3 周) 可抑制 PA1280、GA6201 和 LU2505 异种移植小鼠模型中的肿瘤生长[1]。

Odafosfamide (2.5 mg/kg，腹腔注射，每周一次，3 周) 在儿童 ALL 的 PDX 小鼠模型中诱导疾病明显且长期消退[2]。

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

Animal Model: HepG2 orthotopic xenograft (~1 mm3 in diameter) female athymic nude mice (6 weeks; BALB/c-nu) model[1]
Dosage: 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg
Administration: i.v., once a week, 2 weeks
Result: Inhibited tumor growth, with growth inhibition (TGI) at Day 34 of 52.4% at 1.25 mg/kg, 91.5% at 2.5 mg/kg and 101.2% at 5 mg/kg, respectively.
Animal Model: (CRPC) VCaP xenograft male BALB/c nude mice model[1]
Dosage: 2.5 mg/kg, 5 mg/kg
Administration: i.v., weekly for 5 doses
Result: Inhibited tumor growth, with growth inhibition of 148% at 5 mg/kg, further enhanced to 158% when combined with Abiraterone (HY-70013)/Prednisolone (HY-17463).
Animal Model: PDX (female 20–25 g) NSG mice models of pediatric ALL[2]
Dosage: 2.5 mg/kg
Administration: i.p., once weekly × 3 weeks
Result: Induced substantial and prolonged regressions of disease in All-8, ALL-27, ALL-29, ALL-30, ALL-31, ALL-28,ALL-AKR1C3, combined with Nelarabine (HY-13701) resulted in prolongation of mouse EFS compared with each single agent alone.
分子量

460.42

Formula

C21H25N4O6P
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

Odafosfamide 相关分类

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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:

Odafosfamide2097713-69-2(S)-OBI-3424(S)-TH-3424 AST-3424AST3424AST 3424AST-342417β-HSD17beta-HSD17β-hydroxysteroid dehydrogenases17 beta-hydroxysteroid dehydrogenaseLiver cancerLung cancerleukemialiver cancer cellsNSCLCPDX modelsInhibitorinhibitorinhibit

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