1. Protein Tyrosine Kinase/RTK
  2. Src VEGFR PDGFR FGFR
  3. TG 100572

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 nM。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 TG 100572 Hydrochloride 通常具有更好的水溶性和稳定性。

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TG 100572 Chemical Structure

TG 100572 Chemical Structure

CAS No. : 867334-05-2

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规格 是否有货
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100 mg   询价  
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TG 100572 的其他形式现货产品:

Other Forms of TG 100572:

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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 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 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

IC50 & Target[1]

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 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[1]. TG 100572 is shown to inhibit hRMVEC cell proliferation, with an IC50 of 610±72 nM. This suggests that TG 100572 has the therapeutic potential to inhibit VEGF function in ocular endothelial cells, a contributing factor to pathological angiogenesis in diseases such as AMD and PDR[2].

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

体内研究
(In Vivo)

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[1]. 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[2].

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

分子量

475.97

Formula

C26H26ClN5O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 150 mg/mL (315.15 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1010 mL 10.5049 mL 21.0097 mL
5 mM 0.4202 mL 2.1010 mL 4.2019 mL
查看完整储备液配制表
  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Cell Assay
[1]

For proliferation assays, human retinal microvascular EC plated in 96-well cluster plates are cultured for 48 hr in the presence of either TG 100572 (2 nM-5 µM) or DMSO; medium contained 10% FBS, 50 µg/mL heparin, and 50 ng/mL rhVEGF. Cell numbers are then assessed using an XTT-based assay[1].

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

Animal Administration
[1]

Mice: C57BL/6 mice (15-20 g) are dosed i.p. twice daily for 4 days with 5 mg/ kg TG 100572, followed by a single dose on Day 5, 5 hr after which plasma samples are taken, animals euthanized, and eyes explanted. Alternatively, mice are dosed topically with either TG 100572 or related prodrugs (e.g., TG 100801) by delivering a single 10 µL drop to both eyes for a total of two days, and both plasma and eyes harvested prior to or 0.5, 1, 3, 5, or 7 hr after the Day 2 dosing[1].

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

参考文献

完整储备液配制表

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1010 mL 10.5049 mL 21.0097 mL 52.5243 mL
5 mM 0.4202 mL 2.1010 mL 4.2019 mL 10.5049 mL
10 mM 0.2101 mL 1.0505 mL 2.1010 mL 5.2524 mL
15 mM 0.1401 mL 0.7003 mL 1.4006 mL 3.5016 mL
20 mM 0.1050 mL 0.5252 mL 1.0505 mL 2.6262 mL
25 mM 0.0840 mL 0.4202 mL 0.8404 mL 2.1010 mL
30 mM 0.0700 mL 0.3502 mL 0.7003 mL 1.7508 mL
40 mM 0.0525 mL 0.2626 mL 0.5252 mL 1.3131 mL
50 mM 0.0420 mL 0.2101 mL 0.4202 mL 1.0505 mL
60 mM 0.0350 mL 0.1751 mL 0.3502 mL 0.8754 mL
80 mM 0.0263 mL 0.1313 mL 0.2626 mL 0.6566 mL
100 mM 0.0210 mL 0.1050 mL 0.2101 mL 0.5252 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
TG 100572
目录号:
HY-10184
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