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ACTB-1003 (Synonyms: ACTB-1003)
目录号: PC16106 纯度: ≥98%
CAS No. :939805-30-8
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中文名称
ACTB-1003
中文别名
N-[4-[4-氨基-6-(甲氧基甲基)-7-(4-吗啉基甲基)吡咯并[2,1-F][1,2,4]三嗪-5-基]-2-氟苯基]-N'-[2-氟-5-(三氟甲基)苯基]脲
英文名称
ACTB-1003
英文别名
ACTB-1003;44750KD9OE;1-[4-[4-amino-6-(methoxymethyl)-7-(morpholin-4-ylmethyl)pyrrolo[2,1-f][1,2,4]triazin-5-yl]-2-fluorophenyl]-3-[2-fluoro-5-(trifluoromethyl)phenyl]urea;BCP13578;SB17196;Urea, N-(4-(4-amino-6-(methoxymethyl)-7-(4-morpholinylmethyl)pyrrolo(2,1-F)(1,2,4)triazin-5-yl)-2-fluorophenyl)-N'-(2-fluoro-5-(trifluoromethyl)phenyl)-;A14431;N-[4-[
Cas No.
939805-30-8
分子式
C27H26F5N7O3
分子量
591.53
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.

性状

Solid

IC50 & Target[1][2]

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.

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

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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : ≥ 35 mg/mL (59.17 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6905 mL 8.4527 mL 16.9053 mL
5 mM 0.3381 mL 1.6905 mL 3.3811 mL
10 mM 0.1691 mL 0.8453 mL 1.6905 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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