flt-3-in-3

FLT3-IN-3 是 FLT3抑制剂，能够抑制 FLT3 WT (IC50:13 nM) 和 FLT3 D835Y (IC50:8 nM) 。

JAK2 FLT3-IN-3 (11r) 作为一种针对FLT3和JAK2的双重抑制剂,其IC50值显示,对JAK2、FLT3和JAK3的抑制作用分别达到2.01 nM、0.51 nM和104.40 nM.此化合物能有效诱导凋亡并展现出抗癌活性.

OSI-930 是 Kit，KDR 和 CSF-1R (c-Fms)的口服选择性抑制剂，IC50分别为 80 nM，9 nM 和 15 nM。它具有抗肿瘤活性，靶向肿瘤中的癌细胞增殖和血管生成。它还适度抑制 Flt-1，c-Raf 和 Lck，并且对 PDGFRα β，Flt-3和 Abl 具有较弱的抑制活性。

FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD (FLT3 mutation) with an IC50 of 1.336 nM.

FLT3-IN-2 是 FLT3 抑制剂(IC50＜1 μM)。

FLT3 ligand-2 是PROTAC中的靶蛋白配体 (Ligand for Target Protein for PROTAC)，可用于合成PROTAC FLT-3 degrader 1。

BPR1-J097 是新型的、强效的FLT3抑制剂 (IC50:11 nM)。

Flt3 Inhibitor IV is a potent ATP-competitive Flt3 inhibitor.

Desmorpholinyl Quizartinib-PEG2-COOH is a compound featuring an FLT-3 ligand and a PEG-based PROTAC linker. It is employed in the synthesis of PROTAC FLT-3 degrader 1, which serves as a degrader for the FLT-3 internal tandem duplication (ITD) through PROTAC technology. The degrader exhibits an IC50 of 0.6 nM.

BPR1J-097 hydrochloride (1327167-19-0(free base)) 是一种新型小分子 FLT-3抑制剂(IC50=11±7 nM)，具有很好的体内抗肿瘤活性。

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......

Emirodatamab (AMG-427) 为一种具备延长半衰期的抗FLT3 CD3双特异性T细胞接合剂。该化合物能强效诱导原发性AML母细胞的细胞毒性，并提升FLT-3表达水平。结合抗PD-1抗体后，Emirodatamab的T细胞依赖性细胞毒性（TDCC）得以增强。此外，该化合物亦适用于进行复发或难治性AML的相关研究。