OBI-3424(Synonyms: TH-3424)

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OBI-3424 (Synonyms: TH-3424) 纯度: 99.23%

OBI-3424 (TH-3424) 是一种前药,可通过 AKR1C3 (醛基酮还原酶 1C3) 选择性地转化为有效的 DNA 烷基化剂。OBI-3424 可用于肝细胞癌,去势抵抗性前列腺癌和急性淋巴细胞白血病 (ALL) 的研究。

OBI-3424(Synonyms: TH-3424)

OBI-3424 Chemical Structure

CAS No. : 2097713-68-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4560 In-stock
5 mg ¥4500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

OBI-3424 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

OBI-3424 (TH-3424) is a prodrug that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research[1].

体外研究
(In Vitro)

OBI-3424 exerts potent cytotoxicity against the H460 lung cancer cell line (IC50 of 4.0 nM). OBI-3424 exhibits potent cytotoxicity, in particular against cell lines derived from T-ALL with high AKR1C3 expression, with IC50 values in the low nM range[1].
OBI-3424 also exerts potent cell killing against ALL PDXs, and the median IC50 values were 60.3 nM for B-ALL, 9.7 nM for T-ALL and 31.5 nM for ETP-ALL[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

OBI-3424 (0.5-2.5 mg/kg; i.p.; once weekly; for 3 weeks) treatment induces regressions in PDXs mice and results in prolongation of mouse event-free survival[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NSG mice (20-25 g) bearing patient-derived xenografts (PDX)[1]
Dosage: 0.5 mg/kg, 1 mg/kg, 2.5 mg/kg
Administration: Intraperitoneal injection; once weekly; for 3 weeks
Result: Resulted in prolongation of mouse event-free survival.

Clinical Trial

分子量

460.42

Formula

C21H25N4O6P

CAS 号

2097713-68-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (108.60 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1719 mL 10.8596 mL 21.7193 mL
5 mM 0.4344 mL 2.1719 mL 4.3439 mL
10 mM 0.2172 mL 1.0860 mL 2.1719 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (10.86 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (10.86 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.43 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Kathryn Evans, et al. OBI-3424, a Novel AKR1C3-Activated Prodrug, Exhibits Potent Efficacy against Preclinical Models of T-ALL. Clin Cancer Res. 2019 Jul 15;25(14):4493-4503.

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