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EOC317
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。
EOC317图片
CAS NO:939805-30-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
ACTB-1003
产品介绍
EOC317 (ACTB-1003) 是口服可用的激酶抑制剂,抑制FGFR1VEGFR2Tie-2IC50值分别为6,2 和 4 nM。
生物活性

EOC317 (ACTB-1003) is an oral kinase inhibitor withIC50s of 6, 2 and 4 nM forFGFR1,VEGFR2andTie-2.

IC50& Target[1]

FGFR1

6 nM (IC50)

VEGFR2

2 nM (IC50)

Tie-2

4 nM (IC50)

体外研究
(In Vitro)

EOC317 (ACTB-1003) is an oral kinase inhibitor with multiple modes of action, targeting cancer mutations via FGFR inhibition FGFR1 (IC50=6 nM), angiogenesis through inhibition of VEGFR2 (2 nM), Tie-2 (4 nM), and induces apoptosis likely by targeting RSK (5 nM) and p70S6K (32 nM). EOC317 is highly active with dose-dependent tumor growth inhibition in cell lines with FGFR genetic alterations-OPM2 human multiple myeloma and the murine leukemia Ba/F3-TEL-FGFR1. OPM2 cells harbor the FGFR3 t(4:14) translocation, FGFR3 K650E mutation and PTEN deletion while the Ba/F3-TEL-FGFR1 cells are driven by FGFR1 over-expression[1].

体内研究
(In Vivo)

EOC317 (ACTB-1003) is shown to inhibit tumor angiogenesis evident by the inhibition of CD31 staining in tumor sections. EOC317 is combinable with 5-FU or paclitaxel without diminishing the activity or increasing the toxicity of these chemotherapy agents in the HCT-116 colon tumor xenograft model[1].

Clinical Trial
分子量

591.53

性状

Solid

Formula

C27H26F5N7O3

CAS 号

939805-30-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 35 mg/mL(59.17 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.6905 mL8.4527 mL16.9053 mL
5 mM0.3381 mL1.6905 mL3.3811 mL
10 mM0.1691 mL0.8453 mL1.6905 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。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。