Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T38562 |
AKN-028
|
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
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。 | |||
T7673 |
ATH686
ATH 686 |
Apoptosis; FLT | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
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。 | |||
T1667 |
Tandutinib
MLN518,CT53518,NSC726292,坦度替尼 |
Apoptosis; FLT; CSF-1R; PDGFR; Src; c-Kit | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
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。 | |||
T12610L |
3-Hydroxy Midostaurin
CGP52421 |
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
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]. | |||
T32288 |
JH-IX-179
JH-IX179,JH-IX 179 |
||
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 | |||
T19119 |
3-Hydroxy Midostaurin-D5
CGP52421-D5 |
Others | Others |
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). | |||
T61358 | AKN-028 acetate | ||
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。 | |||
T68389 | LY2457546 | ||
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 synge... |