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Cat. No. Product Name Target Signaling Pathways
T2066 Quizartinib

AC220,奎扎替尼

Apoptosis; FLT; Autophagy; Ligands for Target Protein for PROTAC Angiogenesis; Apoptosis; Autophagy; PROTAC; Tyrosine Kinase/Adaptors
Quizartinib (AC220) 是一种具有口服活性的高选择性Ⅱ 型 FLT3酪氨酸激酶抑制剂,可诱导细胞凋亡。它抑制 Wt FLT3 和 突变型 FLT3-ITD 自磷酸化,IC50分别为 4.1 nM 和 1.1 nM。它可通过优化的 linker 与 VHL 配体连接,从而形成 PROTAC Flt3 降解剂。
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。
T62824 FLT3/ITD-IN-3

FLT3/ITD-IN-3 (Compound 19) 是一种 FLT3-ITD 的有效抑制剂,能够作用于 FLT3D835Y (IC50: 0.3 nM)、FLT3 (IC50: 0.4 nM) 和 FLT3-ITD (IC50: 0.9 nM)。 FLT3/ITD-IN-3FLT3 的磷酸化显示出有效抑制作用,能够有效抗急性髓系白血病细胞的增殖。
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].
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。
T63274 FLT3/ITD-IN-2

FLT3/ITD-IN-2 是 FLT3-ITD 的有效抑制剂,能够作用于 FLT3D835Y (IC50: 0.3 nM)、FLT3(IC50: 0.4 nM)和 FLT3-ITD(IC50: 1.0 nM)。FLT3/ITD-IN-2 能够有效的抑制 FLT3 的磷酸化,能够有效的抑制急性髓系白血病细胞的增殖。
T63127 PDGFRα/FLT3-ITD-IN-3

PDGFRα/FLT3-ITD-IN-3 (Compound 18d) 是一种有效的 PDGFRα (IC50: 0.153 μM)、FLT3 (IC50: 0.004 μM) 抑制剂。PDGFRα/FLT3-ITD-IN-3 具有潜力进行急性髓系白血病或慢性嗜酸性粒细胞白血病的研究。
T63629 PDGFRα/FLT3-ITD-IN-2

PDGFRα/FLT3-ITD-IN-2 是 PDGFRα (IC50>20 μM) 和 FLT3 (IC50: 0.004 μM) 的有效抑制剂。PDGFRα/FLT3-ITD-IN-2 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。
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。
T71857 GTP-14564

FLT; Tyrosine Kinases Angiogenesis; Tyrosine Kinase/Adaptors
GTP-14564是一种新型酪氨酸激酶抑制剂,对 wt-FLT3ITD-FLT3也具有抑制作用。GTP-14564 在 3μ m 处抑制表达 ITD-FLT3 的白细胞介素-3 非依赖性 Ba/F1 的生长,而需要高 30 倍的 GTP-14564 浓度来抑制表达野生型 FLT3 的 Ba/F3FLT3 配体依赖性生长 (wt-FLT3)。
T9428 HM43239

FLT Angiogenesis; Tyrosine Kinase/Adaptors
HM43239 是一种具有口服活性和选择性 FLT3抑制剂,IC50值为 1.1 nM (FLT3 野生型)、1.8 nM (FLT3 ITD 突变型) 和 1.0 nM (FLT3 D835Y 突变型)。HM43239 作为可逆的 I 型抑制剂直接抑制 FLT3 的激酶活性,并调节 p-STAT5, p-ERK SYK, JAK1/2 和 TAK1。HM43239 抑制白血病细胞的增殖并诱导其凋亡 (apoptosis)。
T77763 Wu-5

DUB Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
Wu-5 是一种有效的 USP10 抑制剂,对 FLT3 和 AMPK 通路有抑制作用,促使 FLT3-ITD 分解并诱导细胞凋亡(apoptosis)。
T27011 CHMFL-FLT3-122

CHMFLFLT3122,CHMFL FLT3 122

FLT Angiogenesis; Tyrosine Kinase/Adaptors
CHMFL-FLT3-122 是一种强效口服 FLT3 激酶抑制剂,用于治疗 FLT3-ITD 阳性急性髓性白血病。CHMFL-FLT3-122能显著抑制 MV4-11细胞异种移植模型(50 mg/kg)的肿瘤生长,且在体内无明显毒性。
T1744 BIX02188

Apoptosis; MEK Apoptosis; MAPK
BIX02188 是一种具有选择性和有效性的 MEK5 抑制剂,抑制 MEK5 诱导表达致癌突变体FLT3-ITD的细胞凋亡。
T4428 CCT241736

FLT; Aurora Kinase Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
CCT241736 是一种口服生物可利用的双重 FLT3/Aurora 激酶抑制剂,还抑制临床相关的 FLT3 耐药突变体,包括 FLT3-ITDFLT3。它是 CCT137690 的高级类似物,是治疗人类恶性肿瘤的临床前开发候选物。
T10622 BSc5371

Others Others
BSc5371 is a potent and irreversible FLT3 inhibitor (Kds: 1.3, 0.83, 1.5, 5.8, and 2.3 nM for mutant FLT3 D835H, FLT3 ITD/D835V, FLT3 ITD/F691L, FLT3-ITD, and wild type FLT3 wt).
T11300 FLT3-IN-6

Others Others
FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD (FLT3 mutation) with an IC50 of 1.336 nM.
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)。
T79490 LT-540-717

LT-540-717(化合物32)作为一款有效的FLT3抑制剂(IC50=0.62 nM),展现出抗增殖活性。此外,LT-540-717 抑制多个获得性FLT3突变型,包括FLT3 (ITD, D835V)、FLT3 (ITD, F691L)、FLT3 (D835Y) 及FLT3(D835V),显示其作为抗AML剂的潜力。
T63058 FLT3-IN-14

FLT3-IN-14 是一种 FLT3 的有效抑制剂,能够作用于 FLT3-WT (IC50: 5.6 nM) 和 FLT3-ITD (IC50: 1.4 nM)。FLT3-IN-14 能够抑制 FLT3 (Y591) 磷酸化,将细胞周期停滞在 G1 期并诱导细胞凋亡。
T70597 G-749 hydrochloride

G-749 hydrochloride is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays.
T61758 HP1328

HP1328 is a highly effective inhibitor of FLT3 receptor tyrosine kinase with a specific focus on FLT3/ITD mutation. It belongs to the benzoimidazole scaffold-based compound family. Significantly reducing the leukemia burden, HP1328 effectively extends the survival of mice afflicted with FLT3/ITD leukemia [1].
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...
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。
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FLT3ITD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。
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。
T74707 PROTAC FLT3/CDK9 degrader-1

PROTACFLT3/CDK9 degrader-1 是一种有效的FLT3和CDK9双PROTAC 降解剂。PROTACFLT3/CDK9 degrader-1 诱导细胞凋亡 (Apoptosis) 并有效降解靶蛋白FLT3和 CDK9。PROTACFLT3/CDK9 degrader-1具有研究 FLT3-ITD 突变型 AML 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。
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].
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。
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。
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。
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。
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...
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
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。
T39085 SEL24-B489

SEL24-B489

SEL24-B489 is a highly effective and orally bioavailable compound that acts as a robust, type I inhibitor of both PIM and FLT3-ITD. It exhibits exceptional binding affinity with K d values of 2 nM for PIM1, 2 nM for PIM2, and 3 nM for PIM3.
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)。
T79322 Antiproliferative agent-30

Antiproliferative agent-30 (Compound 8g) 抑制微管蛋白组装且可抑制FLT3及Abl1。该化合物展现出对血管的破坏活性,并对多种癌细胞系表现出强效的抗增殖能力,包括HCT-116、K562及MV-4-11细胞(IC50值分别为0.054 nM、0.008 nM、0.144 nM)。此外,Antiproliferative agent-30 亦对携带FLT3-ITD-TKD突变的AML显示出抗癌效果。
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%。
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].
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 ...
T70446 Abivertinib HCl

Abivertinib, also known as AC0010 and Avitinib, is a third-generation EGFR tyrosine kinase inhibitor and BTK Inhibitor that demonstrated clinical efficacy and manageable adverse events (AEs). Abivertinib inhibits cell proliferation, reduces colony-forming capacity, and induces apoptosis and cell cycle arrest in AML cells, especially those harboring FLT3-ITD mutations. Abivertinib was also found to be more sensitive than ibrutinib in treating AML. Abivertinib may be a promising novel agent for A...
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...
T62417 MELK-8a

MELK-8a (NVS-MELK8a) 是一种高效的、选择性的母体胚胎亮氨酸拉链激酶 (MELK) 抑制剂 (IC50: 2 nM)。MELK-8a 也能够抑制 Flt3 (ITD) (IC50: 0.18 μM)、Haspin (IC50: 0.19 μM)、PDGFRα (IC50: 0.42 μM)。其中 MELK 在调节癌细胞的细胞有丝分裂中具有重要作用。
T12555 PROTAC FLT-3 degrader 1

Others Others
PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.

化合物

Quizartinib
Cat.No: T2066
Synonym: AC220,奎扎替尼
Target: Apoptosis, FLT, Autophagy, Ligands for Target Protein for PROTAC
Tandutinib
Cat.No: T1667
Synonym: MLN518,CT53518,NSC726292,坦度替尼
Target: Apoptosis, FLT, CSF-1R, PDGFR, Src, c-Kit
FLT3/ITD-IN-3
Cat.No: T62824
Synonym:
Target:
FLT3/ITD-IN-1
Cat.No: T61415
Synonym:
Target:
FLT3/ITD-IN-4
Cat.No: T62863
Synonym:
Target:
FLT3/ITD-IN-2
Cat.No: T63274
Synonym:
Target:
PDGFRα/FLT3-ITD-IN-3
Cat.No: T63127
Synonym:
Target:
PDGFRα/FLT3-ITD-IN-2
Cat.No: T63629
Synonym:
Target:
PDGFRα/FLT3-ITD-IN-1
Cat.No: T63454
Synonym:
Target:
GTP-14564
Cat.No: T71857
Synonym:
Target: FLT, Tyrosine Kinases
HM43239
Cat.No: T9428
Synonym:
Target: FLT
Wu-5
Cat.No: T77763
Synonym:
Target: DUB
CHMFL-FLT3-122
Cat.No: T27011
Synonym: CHMFLFLT3122,CHMFL FLT3 122
Target: FLT
BIX02188
Cat.No: T1744
Synonym:
Target: Apoptosis, MEK
CCT241736
Cat.No: T4428
Synonym:
Target: FLT, Aurora Kinase
BSc5371
Cat.No: T10622
Synonym:
Target: Others
FLT3-IN-6
Cat.No: T11300
Synonym:
Target: Others
SKLB4771
Cat.No: T2051
Synonym: FLT3-​IN-​1,FLT3-IN-1
Target: FLT
LT-540-717
Cat.No: T79490
Synonym:
Target:
FLT3-IN-14
Cat.No: T63058
Synonym:
Target:
G-749 hydrochloride
Cat.No: T70597
Synonym:
Target:
HP1328
Cat.No: T61758
Synonym:
Target:
Sorafenib N-oxide
Cat.No: T36681
Synonym:
Target:
FLT3-IN-20
Cat.No: T79596
Synonym:
Target:
PHI-101
Cat.No: T81490
Synonym:
Target:
Pomalidomide-C5-Dovitinib
Cat.No: T81421
Synonym:
Target: PROTACs
PROTAC FLT3/CDK9 degrader-1
Cat.No: T74707
Synonym:
Target:
HDAC10-IN-1
Cat.No: T60794
Synonym:
Target:
HP1142
Cat.No: T61329
Synonym:
Target:
PF15
Cat.No: T74259
Synonym:
Target: PROTACs
PF15 TFA
Cat.No: T77932
Synonym:
Target: PROTACs
FLT3/TrKA-IN-1
Cat.No: T62801
Synonym:
Target:
FLT3-IN-23
Cat.No: T82392
Synonym:
Target:
BPR1J-340
Cat.No: T70779
Synonym:
Target:
JH-IX-179
Cat.No: T32288
Synonym: JH-IX179,JH-IX 179
Target:
HDAC10-IN-2 hydrochloride
Cat.No: T78145
Synonym:
Target: Autophagy
SEL24-B489
Cat.No: T39085
Synonym: SEL24-B489
Target:
HDAC10-IN-2
Cat.No: T60760
Synonym:
Target:
Antiproliferative agent-30
Cat.No: T79322
Synonym:
Target:
FLT3-IN-21
Cat.No: T79391
Synonym:
Target:
AC-4-130
Cat.No: T35429
Synonym:
Target:
FI-700
Cat.No: T68497
Synonym:
Target:
Abivertinib HCl
Cat.No: T70446
Synonym:
Target:
LY2457546
Cat.No: T68389
Synonym:
Target:
MELK-8a
Cat.No: T62417
Synonym:
Target:
PROTAC FLT-3 degrader 1
Cat.No: T12555
Synonym:
Target: Others
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