eph inhibitor-2

Eph inhibitor 2 是一种 Eph 家族酪氨酸激酶抑制剂。

SI-2 hydrochloride (EPH 116 hydrochloride) 是 SRC-3 的抑制剂，诱导乳腺癌细胞死亡的 IC50 值为 3-20 nM。SI-2 hydrochloride 具有良好的药代动力学特征和改善的毒性，以及可接受的口服可用性。

Ehp-inhibitor-2 是一种靶向 Eph 受体的 Eph 家族酪氨酸激酶抑制剂。

LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 syngeneic rat mammary tumor models. Additionally, LY2457546 caused complete regression of well-established tumors in an acute myelogenous leukemia (AML) FLT3-ITD mutant xenograft tumor model. The unique spectrum of target activity, potent in vivo anti-tumor efficacy in a variety of rodent and human solid tumor models, exquisite potency against a clinically relevant model of AML, and non-clinical safety profile justify the advancement of LY2457546 into clinical testing. (source: Invest New D......