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网站主页 化工产品目录 生物化工 生化试剂 激动剂抑制剂 1018069-81-2 化合物 TG 100801 Hydrochloride
  • 化合物 TG 100801 Hydrochloride|T13157L|TargetMol

化合物 TG 100801 Hydrochloride|T13157L|TargetMol

TG 100801 Hydrochloride
1018069-81-2
￥17500 100mg 起订
￥10600 25mg 起订
￥13800 50mg 起订
上海 更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐
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邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 TG 100801 Hydrochloride
英文名称：
TG 100801 Hydrochloride
CAS号：
1018069-81-2
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
产品类别：
抑制剂
货号：
T13157L

Product Introduction

Bioactivity

名称TG 100801 Hydrochloride
描述TG 100801 Hydrochloride is a prodrug to treat age-related macular degeneration. TG 100572 is a inhibitor of multi-targeted kinase(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).
体外活性TG 100801 is readily converted to the active TG 100572 in the eye.TG 100572 is shown to inhibit hRMVEC cell proliferation(IC50 of 610±72 nM)[1]. TG 100801 is formed by derivitization of a phenolic moiety in TG100572 to yield an ester. It displays excellent balance of stability (physical and chemical) with hydrolysis rate. On its own, TG 100801 does not display meaningful anti-kinase activity, as the ester group blocks key interactions with kinase active sites, however exposure to esterases (abundant in mammalian tissues) rapidly liberates active TG100572.TG 100572 shows sub-nanomolar activity against the Src family as well as RTK such as VEGFR1 and R2, FGFR1 and R2, and PDGFRβ. vascular endothelial cell proliferation with ED50 of 610±71 nM inhibited by TG 100572 and blocks VEGF-induced phosphorylation of extracellular signal-regulated kinase[2].
体内活性A concentration of 23.4 μM (Cmax) of TG 100572 is reached in 30 min (Tmax)=0.5 h) in the choroid and the sclera. However, the levels of TG 100572 in the retina are relatively low. The half-life of TG 100572 in ocular tissues is very short; hence, the compound is administered topically minimum t.i.d. to maintain appropriate drug levels in the eye. The maximum concentration one can achieve in formulations using TG 100572 is 0.7% w/v[1]. TG 100801 nor TG100572 are detectable in plasma following topical delivery of TG 100801, and adverse safety signals (such as weight loss) are not observed even with prolonged dosing schedules. Topical TG 100801 significantly suppresses laser-induced choroidal neovascularlization in mice, and reduces fluorescein leakage from the vasculature and retinal thickening measured by optical coherence tomography in a rat model or retinal vein occlusion.In a murine model of laser-induced choroidal neovascularization (CNV), Systemic delivery of TG 100572 causes significant suppression of CNV, but with an associated weight loss suggestive of systemic toxicity[2].
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 5 mg/mL (8.11 mM), Sonication is recommended.
关键字TG-100801 Hydrochloride | TG100801 Hydrochloride | TG 100801 Hydrochloride
相关产品Ribociclib | Lenvatinib | Axitinib | Sorafenib tosylate | Lenvatinib mesylate | Sanguinarine chloride | Regorafenib | Pazopanib | Nintedanib | Sorafenib | Regorafenib monohydrate | Nintedanib esylate
TG 100801 Hydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

化合物 TG 100801 Hydrochloride相关厂家报价

  • TG-101348;
  • TG-101348;
  • 湖北诺迪纳生物技术有限公司 VIP
  • 2024-11-20
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