PTC299|1256565-36-2|-陌孚医药/Medlife

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PTC299

目录号: PL02678 纯度: ≥99%

CAS No. :1256565-36-2

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中文名称	PTC299
英文名称	PTC299
英文别名	(4-Chlorophenyl) (1R)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxyla;PTC299
Cas No.	1256565-36-2
分子式	C₂₅H₂₀Cl₂N₂O₃
分子量	467.34
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

PTC299 是 VEGFA mRNA 翻译的具有口服活性抑制剂，在转录后水平选择性地抑制 VEGF 蛋白的合成。PTC299 也是二氢乳酸盐脱氢酶 (DHODH) 的有效抑制剂。PTC299 良好的口服生物利用度，缺乏脱靶激酶抑制和骨髓抑制。PTC299 可用于血液系统恶性肿瘤的研究。

生物活性

PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies.

性状

Solid

IC50 & Target[1][2]

VEGF

体外研究(In Vitro)

PTC299 inhibits hypoxia-induced VEGFA protein production in HeLa cells with an EC50 of 1.64 ± 0.83 nM.
PTC299 is the most potent inhibitor with an IC50 of about 1 nM, over 10 to 1000-fold more potent than Brequinar, Vidofludimus or A 77-1726 in leukemia cells. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Cao L, et al. Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of DihydroorotateDehydrogenase with Favorable Pharmaceutical Properties. Mol Cancer Ther. 2019 Jan;18(1):3-16.
[2]. Bender Ignacio RA, et al. Brief Report: A Phase 1b/Pharmacokinetic Trial of PTC299, a Novel PostTranscriptional VEGF Inhibitor, for AIDS-Related Kaposis Sarcoma: AIDS Malignancy Consortium Trial 059. J Acquir Immune Defic Syndr. 2016 May 1;72(1):52-7.

溶解度数据	In Vitro: DMSO : 50 mg/mL (106.99 mM; Need ultrasonic)配制储备液

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产品使用指南

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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