1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    FGFR
    PDGFR
    Src
  3. TG 100801

TG 100801 

目录号: HY-10186 纯度: 98.03%
产品使用指南

TG 100801 是TG 100572的前药,通过去酯化产生TG 100572,开可用于黄斑变性的研究。TG 100572 是多靶点激酶抑制剂,抑制受体酪氨酸激酶 (receptor tyrosine kinases) 和Src激酶 (Src kinases); 对VEGFR1,VEGFR2,FGFR1,FGFR2,PDGFRβ,Fgr,Fyn,Hck,Lck,Lyn,Src,Yes 的 IC50 值分别为2,7,2,16,13,5,0.5,6,0.1,0.4,1,0.2。

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TG 100801 Chemical Structure

TG 100801 Chemical Structure

CAS No. : 867331-82-6

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

TG 100801 is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has 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.

IC50 & Target

VEGFR1

2 nM (IC50)

VEGFR2

7 nM (IC50)

FGFR1

2 nM (IC50)

FGFR2

16 nM (IC50)

PDGFRβ

13 nM (IC50)

体外研究
(In Vitro)

TG 100801 is a topically administered prodrug delivered as an eye drop that is readily converted to the active TG 100572 in the eye.TG 100572 is shown to inhibit hRMVEC cell proliferation, with an 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. TG 100572 inhibits vascular endothelial cell proliferation (ED50=610±71 nM) and blocks VEGF-induced phosphorylation of extracellular signal-regulated kinase. TG 100572 induces apoptosis in rapidly proliferating, but not quiescent, endothelial cell cultures[2].

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

体内研究
(In Vivo)

TG 100801 exhibits excellent ocular pharmacokinetics and poor systemic circulation and shows good efficacy in the laser induced choroidal neovascularization model. 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.Systemic delivery of TG 100572 in a murine model of laser-induced choroidal neovascularization (CNV) causes significant suppression of CNV, but with an associated weight loss suggestive of systemic toxicity[2].

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

Clinical Trial
分子量

580.08

Formula

C33H30ClN5O3

CAS 号
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5.56 mg/mL (9.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7239 mL 8.6195 mL 17.2390 mL
5 mM 0.3448 mL 1.7239 mL 3.4478 mL
10 mM --- --- ---
*

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。-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。

参考文献
Animal Administration
[2]

Rats: Long Evans rats are dosed topically in both eyes with 10 µL of TG 100801 (as a 0.3, 0.6 or 1% solution) or vehicle. A total of 5 topical applications are delivered per eye over a three day period: dosing is performed one hour prior to and six hours after laser-induced thrombosis on Day 1, twice on Day 2, and once the morning of Day 3. One hour after the final topical application, retinal edema is assessed by one of two means[2].

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

参考文献

纯度: 98.60%

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
TG 100801
目录号:
HY-10186
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