Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11299 |
FLT3-IN-4
FLT3 inhibitor 9u |
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
FLT3-IN-4 (FLT3 inhibitor 9u) 是一种口服有效的 Fms 样酪氨酸受体激酶 3 (FLT3; IC50= 7 nM) 抑制剂,可用于急性髓性白血病的研究。 | |||
T9856 |
FLT3-IN-10
2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl- |
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
FLT3-IN-10 (2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-) (compound 7c) 是有效的 FMS 样酪氨酸激酶 3 (FLT3) 抑制剂。FLT3-IN-10 具有治疗 FLT3 突变的急性髓性白血病 (AML) 的潜力。 | |||
T62863 |
FLT3/ITD-IN-4
|
||
FLT3/ITD-IN-4 (Compound 16) 是一种选择性的 FLT3 内部串联重复突变 (FLT3-ITD) 抑制剂 (IC50: 2.3 nM)。FLT3/ITD-IN-4 能够用于研究急性骨髓性白血病。 | |||
T67754 |
JAK3-IN-14
|
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
JAK3-IN-14 是一种有效的、选择性的口服活性FLT3抑制剂,对FLT3-WT、FLT3-D835Y 和FLT3-D83H 的IC50分别为~40、8和4nM。 | |||
T64370 |
JI6
JAK3 Inhibitor VI |
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
JI6 (JAK3 Inhibitor VI) 是有效的,选择性的和具有口服活性的 FLT3 抑制剂。JI6抑制 FLT3-WT,FLT3-D835Y 和 FLT3-D835H 的 IC50 值分别为 ~40,8 和 4 nM。JI6 对 JAK3 和 c-Kit 也有抑制作用,IC50 值分别为 ~250 和 ~500 nM。JI6 可用于急性髓性白血病的相关研究。 | |||
T9017 |
HPK1-IN-2
Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2,HPK1-IN-2 |
Others; FLT; Src | Angiogenesis; Others; Tyrosine Kinase/Adaptors |
HPK1-IN-2 (Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2) 是一种有效且具有口服活性的造血祖细胞激酶-1 抑制剂(HPK1;IC50<0.05 µM)。它还抑制 Lck (0.05 µM<IC50<0.5 µM) 和 Flt3 (IC50<0.05 µM) 激酶活性,具有抗肿瘤活性。 | |||
T2500 |
Cediranib
AZD2171,NSC-732208,西地尼布 |
VEGFR; FLT; PDGFR; c-Kit; Autophagy | Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors |
Cediranib (AZD2171) 是一种可口服的高选择性VEGFR2抑制剂,对Flt1、KDR、Flt4、PDGFRα、PDGFRβ和c-Kit 的IC50值分别为小于1、小于3、5、5、36和 2nM。 | |||
T2638 |
Gandotinib
LY2784544 |
VEGFR; FGFR; FLT; JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Gandotinib (LY2784544) 是一种JAK2抑制剂,IC50为 3 nM。它也抑制FLT3、FLT4、FGFR2、TYK2 和 TRKB,IC50分别为 4、25、32、44 和 95 nM。 | |||
T79596 |
FLT3-IN-20
|
||
FLT3-IN-20(compound 34f)作为一种高效FLT3抑制剂,对FLT3-D835Y和FLT3-ITD具有强效性,IC50值分别仅为1 nM和4 nM。该化合物在携带FLT3-ITD突变的AML细胞系MV4-11和MOLM-13中展现出显著的抗增殖效果,其中IC50值分别为7 nM和9 nM;对于带有FLT3-ITD-D835Y突变的MOLM-13变体,其IC50值为4 nM。FLT3-IN-20主要用于肿瘤治疗研究领域。 | |||
T11707 | JAK2/FLT3-IN-1 | JNK | MAPK |
JAK2/FLT3-IN-1 has anti-cancer activity. JAK2/FLT3-IN-1 is a potent and orally effective dual JAK2/FLT3 (Janus kinase 2/ FMS-like tyrosine kinase 3) inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. | |||
T79391 |
FLT3-IN-21
|
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FLT3-IN-21(复合物LC-3)是一种高效的FLT3抑制剂,具有促进细胞凋亡的能力,其对FLT3酶的半抑制浓度(IC50)为8.4 nM。该化合物能够使细胞周期在G1期停滞,并对FLT3-ITD阳性的AML细胞系MV-4-11显示出显著的抑制作用(IC50:5.3 nM)。在小鼠体内,FLT3-IN-21以每日10 mg/kg的剂量可以有效抑制MV-4-11细胞异种移植瘤的生长,肿瘤生长抑制率(TGI)达到92.16%。 | |||
T64104 | JAK2/FLT3-IN-1 TFA | ||
JAK2/FLT3-IN-1 (TFA) 是一种口服具有活力的 JAK2/FLT3 双重抑制剂,表现出抗癌效果,能够作用于 JAK2 (IC50: 0.7 nM),FLT3 (IC50: 4 nM),JAK1 (IC50: 26 nM) 和 JAK3 (IC50: 39 nM)。 | |||
T82393 | FLT3/CHK1-IN-1 | ||
FLT3/CHK-IN-1(Compound 18)为FLT3/CHK1双重抑制剂,其对c-KIT的选择性超1700倍,同时显著降低对hERG的亲和力,IC50为58.4 μM。在MV-4-11细胞接种小鼠异种移植模型中有效抑制肿瘤生长。 | |||
T16995 |
TAS05567
|
FLT; c-RET; JAK; Syk | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR, and RET with IC50s of 10 nM, 4.8 nM, 600 nM, and 29 nM, respectively) in a panel of 192 kinases. | |||
T40097 |
RET-IN-4
|
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RET-IN-4 is a highly effective and specific RET inhibitor that can be administered orally. It demonstrates remarkable potency, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM for inhibiting RET variants including RET (WT), RET (V804M), and RET (M918T), respectively. Moreover, RET-IN-4 exhibits superior selectivity towards kinases JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). Additionally, RET-IN-4 possesses pronounced anticancer properties. | |||
T37085 |
Luxeptinib
|
||
Luxeptinib (CG-806) is a novel pan-FLT3/pan-BTK inhibitor that is administered orally. It exhibits potent and reversible inhibition of these enzymes, acting through a non-covalent mechanism. Luxeptinib effectively induces cell cycle arrest, apoptosis, or autophagy in acute myeloid leukemia cells [1][2][3][4]. | |||
T35429 |
AC-4-130
|
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AC-4-130, a powerful inhibitor of the SH2 domain of STAT5, effectively hinders STAT5 activation, dimerization, nuclear translocation, and transcription of genes reliant on STAT5. This compound directly binds to STAT5, ultimately leading to cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 exhibits notable anti-cancer properties and effectively suppresses abnormal STAT5 activity in acute myeloid leukemia (AML), making it a promising therapeutic option [1]. | |||
T61005 | K783-0308 | ||
K783-0308 是有效的、选择性的MNK2和FLT3的双重抑制剂,IC50值分别为 406 和 680nM。 K783-0308 促进急性髓性白血病 (AML)的 细胞凋亡和细胞周期停滞在 G0/G1 期。K783-0308 抑制 MV-4-11 和 MOLM-13 细胞生长,IC50 值分别为 10.4 和 10.5 μM | |||
T79368 | Antiproliferative agent-34 | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Antiproliferative agent-34 (Compound A14) 是一种多激酶抑制剂,能有效抑制包括EGFRL858R/T790M在内的特定EGFR基因变异形式,IC50为177 nM,对EGFRWT则为1567 nM。它还能抑制JAK2、ROS1、FLT3、FLT4和PDGFRα的活性,其IC50分别为30.93、106.90、108.00、226.60和42.53 nM。在正常氧气环境中,Antiproliferative agent-34对H1975和HCC827细胞株的抑制IC50值低于40 nM,而在低氧环境下,其抑制效能增强4至6倍,IC50值降至低于10 nM。 |