OBI-3424|2097713-68-1|(TH-3424)-陌孚医药/Medlife

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OBI-3424 (Synonyms: TH-3424)

目录号: PL02677 纯度: ≥99%

CAS No. :2097713-68-1

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PL02677-200mg	200mg	询价	询价

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中文名称	OBI-3424
英文名称	OBI-3424
英文别名	3-[5-[(1S)-1-[Bis(aziridin-1-yl)phosphoryloxy]ethyl]-2-nitrophenoxy]-N,N-dimethylbenzamide;(1R)-1-{3-[3-(Dimethylcarbamoyl)phenoxy]-4-nitrophenyl}ethyl bis(1-aziridinyl)phosphinate
Cas No.	2097713-68-1
分子式	C₂₁H₂₅N₄O₆P
分子量	460.42
包装储存	-20°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情

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。

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.

性状

-20°C Solid,>-20°C Oil

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.
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. 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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 50 mg/mL (108.60 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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