EOC317

小分子

EOC317

E647777-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

EOC317 (ACTB-1003) is an oral kinase inhibitor with IC 50 s of 6, 2 and 4 nM for FGFR1 , VEGFR2 and Tie-2 . In Vitro EOC317 (ACTB-1003) is an oral kinase inhibitor with multiple modes of action, targeting cancer mutations via FGFR inhibition FGFR1 (IC 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:FGFR1 6 nM (IC 50 ) VEGFR2 2 nM (IC 50 ) Tie-2 4 nM (IC 50 )

EOC317 (ACTB-1003) 是一种口服激酶抑制剂，对 FGFR1、VEGFR2 和 Tie-2 的 IC 50 s 分别为 6、2 和 4 nM。

939805-30-8

C27H26F5N7O3

591.53 g/mol

23653175

COCC1=C(N2C(=C1C3=CC(=C(C=C3)NC(=O)NC4=C(C=CC(=C4)C(F)(F)F)F)F)C(=NC=N2)N)CN5CCOCC5

COCC1=C(N2C(=C1C3=CC(=C(C=C3)NC(=O)NC4=C(C=CC(=C4)C(F)(F)F)F)F)C(=NC=N2)N)CN5CCOCC5

23653175

DMSO : ≥ 35 mg/mL (59.17 mM)

3

12

7

591.202 Da

591.202 Da

119.000 Ų

42

0

901.000

0

1

2.500