CE-245677

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CE-245677 是一种有效、选择性、口服活性、双重 Tie2/Trk 激酶抑制剂，对于 Tie2 和 TrkA/B 的 IC50 分别为 4.7 nM、1 nM。

CE-245677 is a potent, selective, orally active, dual Tie2/Trk kinase inhibitor with IC50 of 4.7 nM, 1 nM for Tie2 and TrkA/B, respectively; displays >100-fold selectivity against a panel of angiogenic receptor tyrosine kinases (e.g. KDR, PDGFR, FGFR).Pain Phase 1 Clinical.

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50 of 4.7 and 1 nM, and displays >100x selectivity against a number of other angiogenic receptor tyrosine kinases, such as KDR, PDGFR, FGFR.

CE-245677 shows good oral absorption in in vivo rat PK studies (F=80%).

CE245677

Tyrosine Kinase

Angiopoietin Receptor

Angiopoietin Receptor

Neurological Disease

Pain

717899-97-3

513.379

C24H22Cl2N6O3

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (243.48 mM)

O=C(NC1=CC=C(Cl)C=C1Cl)NC2=CC(C(C3=CN(C(C)C)C4=NC=NC(N)=C43)=O)=CC=C2OC

1-(5-(4-amino-7-isopropyl-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonyl)-2-methoxyphenyl)-3-(2,4-dichlorophenyl)urea

(-20℃)

With Ice Pack

≥ 2 years