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TG 100572 Hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TG 100572 Hydrochloride图片
CAS NO:867331-64-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
TG 100572 Hydrochloride 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。
生物活性

TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibitsreceptor tyrosine kinasesandSrckinases; hasIC50s 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 IC50of 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].

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].

分子量

512.43

性状

Solid

Formula

C26H27Cl2N5O2

CAS 号

867331-64-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 25 mg/mL(48.79 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9515 mL9.7574 mL19.5149 mL
5 mM0.3903 mL1.9515 mL3.9030 mL
10 mM0.1951 mL0.9757 mL1.9515 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.88 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。