46
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2051 |
SKLB4771
FLT3-IN-1,FLT3-IN-1 |
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
SKLB4771 (FLT3-IN-1) 是一种新型的、高效的 Flt3 抑制剂 (IC50:10nM)。 | |||
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. | |||
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)。 | |||
T61415 | FLT3/ITD-IN-1 | ||
FLT3/ITD-IN-1 (Compound 1) is a highly potent inhibitor of FLT3 internal tandem duplications (FLT3-ITD). It exhibits remarkable inhibitory effects against FLT3 and FLT3-ITD, with impressive IC50 values of 38.2 nM and 144.1 nM, respectively. Moreover, FLT3/ITD-IN-1 shows exceptional antiproliferative activities against several acute myeloid leukemia cell lines [1]. | |||
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。 | |||
T62801 | FLT3/TrKA-IN-1 | ||
FLT3/TrKA-IN-1 是一种有效的 FLT3/TrKA 双激酶抑制剂,能够作用于 FLT3 (IC50: 43.8 nM)、FLT3-ITD (IC50: 97.2 nM)、FLT3-TKD (IC50: 92.5 nM) 和 TrKA (IC50: 23.6 nM)。FLT3/TrKA-IN-1 能够将细胞周期阻滞在 G0/G1 期,并诱导细胞凋亡 (apoptosis),具有抗增殖作用。FLT3/TrKA-IN-1 具有潜力进行急性髓性白血病 (AML) 的研究。 | |||
T61977 |
FLT3/D835Y-IN-1
|
||
FLT3/D835Y-IN-1 (化合物13a) 是一种选择性的、口服活性的FLT3和FLT3/D835Y 抑制剂,IC50分别为 0.26 nM 和 0.18 nM。FLT3/D835Y-IN-1 具有抗癌作用,可以用于急性髓系白血病的研究。 | |||
T63135 | FLT3/CDK4-IN-1 | ||
FLT3/CDK4-IN-1 是一种高度选择性的、有效的、口服具有活力的 FLT3/CDK4 双重抑制剂,作用于 FLT3 (IC50: 7 nM) 与 CDK4 (IC50: 11 nM)。FLT3/CDK4-IN-1 在体内具有良好的抗肿瘤效果,对某些癌细胞表现出抗增殖作用。 | |||
T63454 |
PDGFRα/FLT3-ITD-IN-1
|
||
PDGFRα/FLT3-ITD-IN-1 是 PDGFRα/FLT3 的有效抑制剂,他们的 IC50 值分别大于 0.036 和 0.003 μM。 PDGFRα/FLT3-ITD-IN-1 对急性髓系白血病或慢性嗜酸性粒细胞白血病表现出研究潜力。 | |||
T1938 |
FLT3-IN-2
|
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
FLT3-IN-2 是 FLT3 抑制剂(IC50<1 μM)。 | |||
T9843 |
FLT3-IN-16
|
||
FLT3-IN-16 是一种有效的FLT3酪氨酸激酶抑制剂,其IC50值为 1.1 μM。FLT3-IN-16 可用于研究急性髓系白血病。 | |||
T4409 |
Gilteritinib
吉列替尼,ASP2215 |
FLT; TAM Receptor; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Gilteritinib (ASP2215) 是一种 FLT3 抑制剂 (IC50:0.29 nM),也是一种 AXL 抑制剂 (IC50:0.73 nM),具有 ATP 竞争性。 | |||
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。 | |||
T3211 |
Midostaurin
米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱 |
Others; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Others |
Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂,有抗肿瘤活性,对 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1/2的IC50值范围为 22 到500 nM 之间。 | |||
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。 | |||
T35900 |
JAK2-IN-7
JAK2-IN-7 |
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK2-IN-7 是一种选择性 JAK2抑制剂,对 JAK2,SET-2 和 Ba/F3V617F 细胞的IC50为 3、11.7 和 41 nM。 JAK2-IN-7 的选择性是 JAK1, JAK3,FLT3 的 14 倍以上。JAK2-IN-7 刺激细胞周期停滞在 G0/G1 期,并诱导肿瘤细胞凋亡 (apoptosis),具有抗肿瘤活性。 | |||
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。 | |||
T78176 |
FLT3-IN-19
|
||
FLT3-IN-19(Comp 50),作为一种选择性FLT3抑制剂,展现出0.213 nM的IC50。适用于AML研究。 | |||
T79420 |
FLT3-IN-22
|
||
FLT3-IN-22(化合物22f)是一款高效的FLT3抑制剂,具有针对FLT3和FLT3/D835Y极低的IC50值,分别为0.941 nM和0.199 nM。在MV4-11细胞和携带FLT3变异的Ba/F3细胞系中(涵盖FLT3-D835Y及FLT3-F691L),此抑制剂显示出显著的抗增殖能力。 | |||
T61101 | FLT3-IN-13 | ||
FLT3-IN-13 (compound 20) is a highly effective inhibitor targeting both topoisomerase II and FLT3 proteins in leukemic cells. It exhibits potent activity against these targets, with IC50 values of 2.26 μM for both. Moreover, FLT3-IN-13 induces cell cycle arrest at the G2/M phase and promotes apoptosis. Notably, it displays considerable anticytotoxic activity, specifically against leukemia [1]. | |||
T82392 | FLT3-IN-23 | ||
FLT3-IN-23作为JFMS样脂氨酸激酶3(FLT3)的抑制剂,表现出7.42 nM的IC50值。该化合物针对带有多种FLT3-TKD与FLT3-ITD-TKD突变的BaF3细胞显示出显著的抗增殖效果。 | |||
T61329 | HP1142 | ||
HP1142 is a highly effective and specific inhibitor targeting the FLT3 receptor tyrosine kinase, with a particular affinity for its mutant variant FLT3/ITD. It exhibits a benzoimidazole scaffold-based structure, making it a promising compound for investigating and studying the FLT3/ITD mutation in the context of leukemia research [1]. | |||
T77932 |
PF15 TFA
|
PROTACs | PROTAC |
PF15 TFA是一种连接FLT3 kinase配体和CRBN配体的PROTAC,作为FLT3-ITD的高选择性降解剂,DC50值为76.7 nM。该化合物可显著抑制FLT3-ITD阳性细胞增殖,并降低FLT3和STAT5磷酸化水平。PF15 TFA亦能抑制小鼠模型的肿瘤生长,并可用于白血病研究。 | |||
T36681 |
Sorafenib N-oxide
|
||
Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibi... | |||
T70779 | BPR1J-340 | ||
BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular proliferation (GC50 approximately 5 nM) assays. BPR1J-340 inhibited the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD(+) AML cells. The pharmacokinetic parameters of BPR1J-340 in rats were determined. BPR1J-340 also demonstrated pronounced tumor growth inhibit... | |||
T74259 | PF15 | PROTACs | PROTAC |
PF15是一种将FLT3 kinase配体与CRBN配体结合的PROTAC,它是FLT3-ITD的高选择性降解剂,显示出76.7 nM的DC50。该化合物能有效抑制FLT3-ITD阳性细胞增殖,并降低FLT3和STAT5的磷酸化水平。在小鼠模型中,PF15也能够抑制肿瘤生长,对白血病研究具有潜在应用价值。 | |||
T68497 |
FI-700
|
||
FI-700 is a novel and potent FLT3 inhibitor with promising antileukemia activity. FI-700 showed a potent IC(50) value against FLT3 kinase at 20 nmol/L in an in vitro kinase assay. FI-700 showed selective growth inhibition against mutant FLT3-expressing leukemia cell lines and primary acute myeloid leukemia cells, whereas it did not affect the FLT3 ligand (FL)-driven growth of Wt-FLT3-expressing cells. Oral administration of FI-700 induced the regression of tumors in a s.c. tumor xenograft model ... | |||
T79391 |
FLT3-IN-21
|
||
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%。 | |||
T81421 |
Pomalidomide-C5-Dovitinib
|
PROTACs | PROTAC |
Pomalidomide-C5-Dovitinib(compound 2)是链接Pomalidomide与Dovitinib的PROTAC,且与CRBN结合。该化合物在FLT3-ITD+ AML细胞中表现出增强的抗增殖能力,通过泛素-蛋白酶体依赖性途径促进FLT3-ITD和KIT蛋白的降解,并彻底抑制其下游信号传导,显示出研究FLT3-ITD+急性髓系白血病的潜力。 | |||
T60794 | HDAC10-IN-1 | ||
HDAC10-IN-1 (化合物 13b) 是一种有效且高选择性的HDAC10抑制剂 (IC 50 = 58 nM),可用于调节侵袭性 FLT3-ITD 阳性急性髓系白血病细胞的自噬。 | |||
T71400 |
Quizartinib HCl
|
||
Quizartinib, also know as AC220 and AC010220, is an orally available FLT3 / STK1 inhibitor with potential antineoplastic activity. Class III receptor tyrosine kinase inhibitor AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell pro... | |||
T21330 |
JNJ-28312141
JNJ 28312141,JNJ28312141 |
||
JNJ-28312141 is an orally active CSF1R inhibitor and a FLT3 inhibitor. JNJ-28312141 is a new agent with potential therapeutic activity in acute myeloid leukemia and in settings where CSF-1-dependent macrophages and osteoclasts contribute to tumor growth a | |||
T78818 | HDAC-IN-63 | ||
HDAC-IN-63(化合物63)是一种针对FLT3和HDAC的双重抑制剂,其中,对FLT3的IC50为0.844 nM,对HDAC1的IC50为30.0 nM。该化合物能有效抑制MV4-11细胞的增殖(IC50为92 nM),在MV4-11细胞中诱导apoptosis并造成细胞周期阻滞。HDAC-IN-63可以应用于急性髓系白血病(AML)的相关研究。 | |||
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]. | |||
T60760 |
HDAC10-IN-2
|
||
HDAC10-IN-2 (化合物 10c) 调节侵袭性 FLT3-ITD 阳性急性髓系白血病细胞的自噬。HDAC10-IN-2是HDAC10的高选择性抑制剂 (IC50 = 20 nM)。 | |||
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。 | |||
T78145 |
HDAC10-IN-2 hydrochloride
|
Autophagy | Autophagy |
HDAC10-IN-2 hydrochloride(化合物10c)是一种对HDAC10具有高效性和高选择性的抑制剂,IC50值为20 nM。该化合物能够调控FLT3-ITD阳性急性髓系白血病细胞的自噬过程。 | |||
T81490 |
PHI-101
|
||
PHI-101是口服FLT3抑制剂,在克服多耐药突变方面表现出高效。该化合物对FLT3的ITD或TKD单突变体表现出显著抑制作用,同时也能抑制包括双重(ITD/D835Y或ITD/F691L)和三重(ITD/D835Y/F691L)耐药突变。PHI-101在治疗复发或难治性急性髓系白血病(AML)的研究中显示出应用潜力。 | |||
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]. | |||
T61755 |
E6201
|
||
E6201 (ER-806201) is a potent dual kinase inhibitor targeting MEK1 and FLT3, inhibiting their activities in an ATP-competitive manner. It effectively suppresses MEK1-induced ERK2 phosphorylation (IC50 = 5.2 nM), MKK4-induced JNK phosphorylation (IC50 = 91 nM), and MKK6-induced p38 MAPK phosphorylation (IC50 = 19 nM). E6201 exhibits anti-tumor and anti-psoriasis effects [1] [2]. | |||
T78871 |
PLM-101
|
||
PLM-101是一种口服抗癌剂,针对FLT3和RET具有选择性抑制作用,有效抑制急性髓系白血病(AML)细胞。通过抑制RET,PLM-101促使FLT3的自噬降解,并且通过抑制PI3K和Ras/ERK信号通路来发挥其抗白血病的活性。在小鼠MV4-11侧翼异种移植模型中,PLM-101以口服剂量3及10 mg/kg显示出抗肿瘤效果,并且在同种异种移植小鼠模型中,剂量为40 mg/kg(口服)亦展现出明显的抗肿瘤功效。 | |||
T35429 |
AC-4-130
|
||
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]. | |||
T73033 | TRK II-IN-1 | Trk receptor | Tyrosine Kinase/Adaptors |
TRKII-IN-1 是一种有效的 II 型TRK抑制剂,对TRKA/B/C及TRKAG667C的IC50分别为3.3、6.4、4.3 和 9.4 nM。此外,TRKII-IN-1 对FLT3、RET和VEGFR2也具有抑制作用,其IC50分别为1.3、9.9 和 71.1 nM。TRKII-IN-1 主要用于TRK驱动的癌症研究。 | |||
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 | |||
T29542 |
AC708
AC 708,AC-708 |
||
AC708 is a small molecule CSF1R inhibitor that effectively inhibits CSF1R phosphorylation mediated by CSF-1 (IC50 = 26 nM) and IL-34 (IC50 = 33 nM). It also inhibited the activity of growth factor-dependent cells cultured in CSF-1 (IC50 = 38 nM) or IL-34 | |||
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S0033 |
Crotonoside
巴豆苷;异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE |
Others; FLT; HDAC | Angiogenesis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Others; Tyrosine Kinase/Adaptors |
Crotonoside (Isoguanosine) 是从中草药巴豆中分离出来的一种天然产物。 它抑制 FLT3 和 HDAC3/6,有治疗急性髓性白血病 (AML)的研究潜力。 |