首页工具

登录

搜索结果

Search Results for " itd 1 "

如果没找到您满意的产品或者您对产品有其他要求，可以联系我们专业顾问为您提供针对性的合理建议。 QQ咨询网站留言咨询

Cat. No.	Product Name	Target	Signaling Pathways
T2273	ITD-1 4-[1,1'-联苯]-4-基-1,4,5,6,7,8-六氢-2,7,7-三甲基-5-氧代-3-喹啉羧酸乙酯	TGF-beta/Smad	Stem Cells
	ITD1 是一个选择性的TGFβ受体抑制剂(IC50:460 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].
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。
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)。
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。
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。
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...
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-FLT3和ITD-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/F3 的 FLT3 配体依赖性生长（wt-FLT3）。
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。
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。
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。
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。
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。
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.
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。
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)。
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。
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。
T39818	Desmorpholinyl Quizartinib-PEG2-COOH Desmorpholinyl Quizartinib-PEG2-COOH
	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.
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...
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].
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%。
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 ...

化合物

Cat.No: T2273

Synonym: 4-[1,1'-联苯]-4-基-1,4,5,6,7,8-六氢-2,7,7-三甲基-5-氧代-3-喹啉羧酸乙酯

Target: TGF-beta/Smad

FLT3/ITD-IN-1

Cat.No: T61415

PDGFRα/FLT3-ITD-IN-1

Cat.No: T63454

Cat.No: T9428

Target: FLT

Cat.No: T60794

Cat.No: T81490

Cat.No: T61758

Sorafenib N-oxide

Cat.No: T36681

Cat.No: T71857

Target: FLT, Tyrosine Kinases

Cat.No: T79596

Pomalidomide-C5-Dovitinib

Cat.No: T81421

Target: PROTACs

Cat.No: T79490

Cat.No: T61329

Cat.No: T77932

Target: PROTACs

PROTAC FLT3/CDK9 degrader-1

Cat.No: T74707

PROTAC FLT-3 degrader 1

Cat.No: T12555

Target: Others

Cat.No: T74259

Target: PROTACs

Cat.No: T60760

HDAC10-IN-2 hydrochloride

Cat.No: T78145

Target: Autophagy

Cat.No: T62801

Cat.No: T82392

Desmorpholinyl Quizartinib-PEG2-COOH

Cat.No: T39818

Synonym: Desmorpholinyl Quizartinib-PEG2-COOH

Cat.No: T70779

Cat.No: T35429

Antiproliferative agent-30

Cat.No: T79322

Cat.No: T79391

Cat.No: T68497

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Copyright © 2015-2024 TargetMol Chemicals Inc. All rights reserved. 沪ICP备20019793号-4

沪公网安备 31010602006700号

沪公网安备 31010602006700号

TargetMol Loading

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼