flt3 autophosphorylation

AKN-028 是酪氨酸激酶 FLT3的抑制剂，可剂量依赖性的诱导 FLT3的自磷酸化。

Quizartinib (AC220) 是一种第二代 Ⅱ 型 FLT3 酪氨酸激酶抑制剂，具有口服活性和高选择性，抑制 FLT3-WT 和 FLT3-ITD 自磷酸化 (IC50=4.1 1.1 nM)。Quizartinib 可以诱导肿瘤细胞凋亡。

3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412[1].

Lestaurtinib (CEP 701) 是一种可口服且具有选择性的 FMS 样酪氨酸激酶-3 （FLT3，IC50：0.9 nM）抑制剂，在体外抑制 FLT3 自磷酸化。Lestaurtinib 促进 c-MYC 表达，可抑制 RPTKs 的磷酸化，对 TrkA 和 JAK2 具有很高的亲和力，可诱导细胞凋亡和细胞生长停滞，可用于研究白血病。

Tandutinib (CT53518) 是一种选择性 FLT3抑制剂，其 IC50为 0.22 μM。它还抑制c-Kit 和PDGFR，其IC50分别为 0.17 μM 和 0.20 μM。它可穿透血脑屏障，用于急性骨髓性白血病。

3-Hydroxy Midostaurin-D5 (CGP52421-D5) is a deuterium-labeled 3-Hydroxy Midostaurin which is a metabolite of PKC412. PKC412 effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation (IC50s: 132 nM and 9.8 μM in culture medium and plasma).

JH-IX-179 is a novel type I ATP competitive and highly selective FLT3 inhibitor. JH-IX-179 is much more selective for FLT3 and FLT3 mutants than for Kronani. In addition, JH-IX-179 showed little human serum protein binding and effectively inhibited autoph

AKN-028 acetate 是一种新型酪氨酸激酶 (TKI) 抑制剂，是一种有效的口服活性的 FMS 样受体酪氨酸激酶 3 (FLT3) 抑制剂，其 IC50值为 6 nM。AKN-028 acetate 抑制 FLT3 自磷酸化。AKN-028 acetate 诱导剂量依赖性的细胞毒性反应 (平均IC50=1 μM)。AKN-028 acetate 通过激活 caspase 3 诱导细胞凋亡 (apoptosis)。AKN-028 acetate 可用于急性髓系白血病 (AML) 的研究。

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......

ATH686 是一种选择性的，ATP 竞争性的FLT3抑制剂，具有抗白血病作用。它靶向突变 FLT3 蛋白激酶活性，并通过诱导凋亡和抑制细胞周期来抑制具有 FLT3 突变的细胞的增殖。