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Search Results for " tyrosine kinase in 1 "

85

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T5466	Tyrosine kinase-IN-1	VEGFR; FGFR; FLT; PDGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	Tyrosine kinase-IN-1是一种多靶点酪氨酸激酶抑制剂，能够抑制KDR (IC50:4 nM)，Flt-1 (IC50:20 nM)，FGFR1 (IC50:4 nM) 和 PDGFRα (IC50:2 nM)。
T14692	BMX-IN-1 BMX kinase inhibitor	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	BMX-IN-1 (BMX kinase inhibitor) 是 X 染色体上的骨髓酪氨酸激酶 (BMX, IC50 = 8 nM) 和相关的布鲁顿酪氨酸激酶 (BTK, IC50 = 10.4 nM) 的特异性抑制剂，但 BMX-IN-1 对 Blk、JAK3、EGFR、Itk 或 Tec 活性的效力要低 47-656 倍以上。
TQ0230	BTK IN-1 SNS062 analog	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	BTK IN-1 (SNS062 analog) (SNS062 analog) 是一种有效的 BTK 抑制剂 (IC50<100 nM)。
T3059	ALK-IN-1 AP26113,Brigatinib,AP26113-analog	EGFR; IGF-1R; ALK	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	ALK-IN-1 (AP26113) 是一种高效的、选择性的 ALK 激酶抑制剂。
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)。
T23504	VEGFR-IN-1 VEGFR Tyrosine Kinase Inhibitor II	Others	Others
	VEGFR inhibitor
T39178	Tyrosine Kinase Peptide 1
	Tyrosine Kinase Peptide 1 is a control substrate peptide for c-Src assay.
T21785	AG957	Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Tyrphostin AG957 是一种酪氨酸激酶抑制剂，具有抗BCR/ABL 酪氨酸激酶活性。它能够抑制p210bcr/abl 酶活性 (IC50:2.9 μM)。
T60220	ROS kinases-IN-1	ROS Kinase	Tyrosine Kinase/Adaptors
	ROS kinases-IN-1 是一种 ROS 酪氨酸激酶抑制剂，IC50 值为 1.22 μM。ROS kinases-IN-1 具有抗肿瘤活性。
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。
T3337	Ddr1-In-1	Discoidin Domain Receptor (DDR)	Tyrosine Kinase/Adaptors
	DDR1-IN-1 是一种特异性的 DDR1 受体酪氨酸激酶抑制剂，选择性是 DDR2 的 3 倍左右。
T3980	Su1498 Tyrphostin SU 1498,AG 1498	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	Su1498 (Tyrphostin SU 1498) 是一种选择性的 VEGFR2 抑制剂，能够抑制 Flk-1 (IC50:700 nM)。
T16730	Remibrutinib	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	Remibrutinib 是有效的、口服具有活力的 bruton tyrosine kinase 抑制剂 (IC50:1 nM)，在血液中抑制 BTK 活性的 IC50的值为 0.23 μM。它具有研究慢性荨麻疹的潜力。
T4075	Sulfatinib KDR-IN-1,索凡替尼	VEGFR; FGFR; HER	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Sulfatinib (KDR-IN-1) (HMPL-012) 是一种有效且高度选择性的酪氨酸激酶抑制剂，可抑制VEGFR1/2/3，FGFR1和CSF1R，IC50范围为1 到 24 nM 之间。
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。
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。
T4182	lavendustin B 薰草菌素B	Tyrosinase; transporter; HIV Protease	Metabolism; Microbiology/Virology; Proteases/Proteasome
	Lavendustin B 是一种酪氨酸激酶抑制剂，是 HIV-1 整合酶 (IN) 与其同源细胞辅助因子、晶状体上皮衍生生长因子 (LEDGF/p75) 相互作用的抑制剂。
T22424	1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea	Apoptosis; STAT	Apoptosis; JAK/STAT signaling; Stem Cells
	SC-1 是一种 Sorafenib 的衍生物，可抑制 STAT3磷酸化，通过依赖 SHP-1 的 STAT3失活诱导细胞凋亡，具有抗癌作用。
T60197	UNC 1025	Others	Others
	UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 ...
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。
T77620	LMTK3-IN-1	c-Met/HGFR	Tyrosine Kinase/Adaptors
	LMTK3-IN-1 是一种有效的 ATP 竞争性狐猴酪氨酸激酶 3 (LMTK3) (Kd=2.5 μM) 抑制剂，通过泛素蛋白酶体途径降解 LMTK3 发挥特性。LMTK3-IN-1 在多种癌细胞系和体内 BC 小鼠模型中展现出抗癌活性。 LMTK3-IN-1（10-20 μM）可诱导 BC 细胞系凋亡。
T63505	Tivozanib hydrochloride hydrate
	Tivozanib hydrochloride hydrate 是选择性的、有效的、口服具有活力的 VEGFR 酪氨酸激酶抑制剂，能够作用于 VEGFR-1 (IC50: 0.21 nM)、VEGFR-2 (IC50: 0.16 nM)、VEGFR-3 (IC50: 0.24 nM)。Tivozanib hydrochloride hydrate 能够抑制肿瘤组织中的血管生成和血管通透性，并具有抗肿瘤作用，对转移性肾细胞癌 (RCC) 具有研究潜力。
T9543	Syk Inhibitor II hydrochloride	Others	Others
	Syk Inhibitor II hydrochloride 信号传导的影响在狼疮中可能很突出。
T10534	BI-4020	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	BI-4020 是一种第四代，口服有效，非共价的 EGFR 酪氨酸激酶抑制剂。BI-4020 表现出对三联突变的 EGFR del19 T790M C797S 突变体 ( BaF3 细胞系，IC50=0.2 nM)，双重突变的 EGFR del19 T790M 以及单突变的 EGFR del19 (IC50=1 nM)的抑制剂活性。BI-4020 保留了抑制 EGFR wt 的活性 (IC50=190 nM)。BI-4020 具有高激酶组选择性和良好的 DMPK 性质。
T61730	Tyrosine kinase-IN-4
	Tyrosine kinase-IN-4 (EXAMPLE 107) 是一种酪氨酸激酶 (tyrosine kinase) 抑制剂。
T39698	Gemnelatinib
	Gemnelatinib (WO2018077227, implementation example 1) is a tyrosine kinase inhibitor with potential applications in cancer research.
T10488	BCR-ABL-IN-1	Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	BCR-ABL-IN-1 is a BCR-ABL tyrosine kinase inhibitor (pIC50: 6.46) and may be used in the research of chronic myelogenous leukemia.
T79612	Tyrosine kinase-IN-6	c-Met/HGFR	Tyrosine Kinase/Adaptors
	Tyrosine kinase-IN-6为RON剪接变异体抑制剂，有效展现抗癌及抗肿瘤活性。
T8888	Lck-IN-1
	Lck-IN-1 是有效的淋巴细胞蛋白酪氨酸激酶(Lck)抑制剂。
T79163	RET-IN-24
	RET-IN-24（Compound 26）为选择性RET酪氨酸激酶抑制剂，具抗肿瘤活性。
T78943	Syk-IN-7	Syk	Angiogenesis; Tyrosine Kinase/Adaptors
	Syk-IN-7（化合物17）是一类特定的酪氨酸激酶（SYK）抑制剂。
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...
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.
T61177	NSC114126
	NSC114126 is a highly effective and orally bioavailable inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR-TK). This compound exhibits robust antiproliferative properties, making it a promising candidate for further investigation in the field of cancer research [1].
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].
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].
T79969	Axl-IN-16	TAM Receptor	Tyrosine Kinase/Adaptors
	Axl-IN-16为Axl与HIF的双效抑制剂，能激发Flammulina velutipes子实体生成，并抑制HIF活性与受体酪氨酸激酶的表达。
T1656L	Vandetanib Fumarate HSDB 8198,Zactima,Caprelsa,ZD 6474,Vandetanib
	Vandetanib Fumarate is an orally available tyrosine kinase inhibitor. Vandetanib Fumarate works by blocking RET (REarranged during Transfection), vascular endothelial growth factor receptor (VEGFR-2, VEGFR-3), and epidermal growth factor receptor and to a
T35915	Erlotinib-13C6 Erlotinib-13C6
	Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1]. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer[1].Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process[2]...
T79859	TIE-2/VEGFR-2 kinase-IN-4
	TIE-2/VEGFR-2 kinase-IN-4，一种苯并咪唑衍生物，作为有效的TIE-2和VEGFR-2酪氨酸激酶受体抑制剂，其IC50值分别为5.2 nM和5.1 nM，适用于血管生成相关研究。
T83218	ABBV-712	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	ABBV-712为选择性酪氨酸激酶 2 (TYK2) 抑制剂，IC50值为0.195 μM，关键作用于自身免疫性疾病。
T78209	Nedometinib	MEK	MAPK
	Nedometinib是MEK1酪氨酸激酶的抑制剂，具备抗肿瘤活性，适用于皮肤病、皮肤纤维神经瘤和神经纤维瘤病研究。
T40785	Gefitinib impurity 1
	Gefitinib impurity 1 is a compound derived from Gefitinib, a potent and selective EGFR tyrosine kinase inhibitor (IC 50 = 33 nM). This orally active compound selectively inhibits tumor cell growth stimulated by EGF (IC 50 = 54 nM) and inhibits EGFR autophosphorylation induced by EGF in tumor cells. Additionally, Gefitinib induces autophagy and exhibits antitumor activity.
T70202	DDR1-IN-1 dihydrochloride
	DDR1-IN-1 dihydrochloride 是 DDR1受体酪氨酸激酶抑制剂，IC50值为105 nM，而对 DDR2的 IC50为413 nM。
T72574	Axl/Mer/CSF1R-IN-1
	Axl/Mer-IN-1 是一种 Axl/Mer 受体酪氨酸激酶 (Axl/Mer RTK) 和CSF1R 抑制剂，Kd 值均小于 0.1 μM。
T79858	TIE-2/VEGFR-2 kinase-IN-3
	TIE-2/VEGFR-2 kinase-IN-3，为苯并咪唑衍生物，具备高效的抑制作用于TIE-2与VEGFR-2受体酪氨酸激酶，其IC50值分别达到6.9 nM和3.5 nM。本化合物主要用于血管生成相关研究。
T28874	SU11652 SU-11652,SU 11652
	SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGFR2, IC50 = 27 nM), FGFR1 (IC50= 170
T35777	Nodularin
	The cyanobacterium Nodularia spumigena often contaminates the drinking water of rural communities in developing countries and accumulates in mussels, flounder, and cod from the northern Baltic Sea. Nodularin is a hepatotoxic monocylic pentapeptide produced by the N. spumigena. It is a potent inhibitor of protein phosphatase types 1 (PP1) and 2A (PP2A), exhibiting IC50 values of 1.8 and 0.026 nM, respectively. PP2B is inhibited to a lesser extent with an IC50 of 1.8 μM. No apparent inhibitory eff...
T67442	CGP-53716
	The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smoo...
T36429	Dihydrodiol-Ibrutinib
	PCI 45227 is an active metabolite of the Bruton's tyrosine kinase inhibitor ibrutinib .1PCI 45227 is formed from ibrutinib by the cytochrome P450 (CYP) isoform CYP3A. 1.Veeraraghavan, S., Viswanadha, S., Thappali, S., et al.Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.107151-158(2015)

化合物

Tyrosine kinase-IN-1

Cat.No: T5466

Target: VEGFR, FGFR, FLT, PDGFR

Cat.No: T14692

Synonym: BMX kinase inhibitor

Target: BTK

Cat.No: TQ0230

Synonym: SNS062 analog

Target: BTK

Cat.No: T3059

Synonym: AP26113,Brigatinib,AP26113-analog

Target: EGFR, IGF-1R, ALK

Cat.No: T2051

Synonym: FLT3-IN-1,FLT3-IN-1

Target: FLT

Cat.No: T23504

Synonym: VEGFR Tyrosine Kinase Inhibitor II

Target: Others

Tyrosine Kinase Peptide 1

Cat.No: T39178

Cat.No: T21785

Target: Bcr-Abl

ROS kinases-IN-1

Cat.No: T60220

Target: ROS Kinase

Cat.No: T4409

Synonym: 吉列替尼,ASP2215

Target: FLT, TAM Receptor, c-Kit

Cat.No: T3337

Target: Discoidin Domain Receptor (DDR)

Cat.No: T3980

Synonym: Tyrphostin SU 1498,AG 1498

Target: VEGFR

Cat.No: T16730

Target: BTK

Cat.No: T4075

Synonym: KDR-IN-1,索凡替尼

Target: VEGFR, FGFR, HER

Cat.No: T9843

Cat.No: T3211

Synonym: 米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱

Target: Others, PKC

Cat.No: T4182

Synonym: 薰草菌素B

Target: Tyrosinase, transporter, HIV Protease

1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea

Cat.No: T22424

Target: Apoptosis, STAT

Cat.No: T60197

Target: Others

Cat.No: T2500

Synonym: AZD2171,NSC-732208,西地尼布

Target: VEGFR, FLT, PDGFR, c-Kit, Autophagy

Cat.No: T77620

Target: c-Met/HGFR

Tivozanib hydrochloride hydrate

Cat.No: T63505

Syk Inhibitor II hydrochloride

Cat.No: T9543

Target: Others

Cat.No: T10534

Target: EGFR

Tyrosine kinase-IN-4

Cat.No: T61730

Cat.No: T39698

Cat.No: T10488

Target: Bcr-Abl

Tyrosine kinase-IN-6

Cat.No: T79612

Target: c-Met/HGFR

Cat.No: T8888

Cat.No: T79163

Cat.No: T78943

Target: Syk

Quizartinib HCl

Cat.No: T71400

Cat.No: T11707

Target: JNK

Cat.No: T61177

Cat.No: T61329

3-Hydroxy Midostaurin

Cat.No: T12610L

Synonym: CGP52421

Target: FLT

Cat.No: T79969

Target: TAM Receptor

Vandetanib Fumarate

Cat.No: T1656L

Synonym: HSDB 8198,Zactima,Caprelsa,ZD 6474,Vandetanib

Cat.No: T35915

Synonym: Erlotinib-13C6

TIE-2/VEGFR-2 kinase-IN-4

Cat.No: T79859

Cat.No: T83218

Target: JAK

Cat.No: T78209

Target: MEK

Gefitinib impurity 1

Cat.No: T40785

DDR1-IN-1 dihydrochloride

Cat.No: T70202

Axl/Mer/CSF1R-IN-1

Cat.No: T72574

TIE-2/VEGFR-2 kinase-IN-3

Cat.No: T79858

Cat.No: T28874

Synonym: SU-11652,SU 11652

Cat.No: T35777

Cat.No: T67442

Dihydrodiol-Ibrutinib

Cat.No: T36429

Cat. No.	Product Name	Target	Signaling Pathways
T3S0027	Picropodophyllotoxin AXL 1717,Picropodophyllin,苦鬼臼毒素	IGF-1R	Tyrosine Kinase/Adaptors
	Picropodophyllotoxin (AXL 1717) 是一种环木脂素生物碱，存在于五月树(Podophyllum peltatum) 中，是一种具有潜在抗肿瘤活性的胰岛素样生长因子 1 受体 (IGF1R) 的小分子抑制剂。它特异性抑制 IGF1R 的活性并下调细胞表达，而不干扰其他生长因子受体的活性，例如胰岛素受体、表皮生长因子、血小板衍生生长因子、成纤维细胞生长因子和肥大/干细胞生长因子 (KIT) ）。该药剂在抑制肿瘤细胞增殖和诱导肿瘤细胞凋亡方面显示出有效的活性。 IGF1R 是一种在多种人类癌症中过度表达的受体酪氨酸激酶，在多种癌细胞的生长和存活中起关键作用。
T83411	2,3,4,6,8-Pentahydroxy-1-methylxanthone
	2,3,4,6,8-Pentahydroxy-1-methylxanthone，一种源自Wardomyces anomalus的山酮衍生物，展示了显著的抗氧化活性，并作为p56lck酪氨酸激酶的抑制剂发挥作用。它在心血管疾病治疗研究中具备潜在应用价值。

天然产物

Picropodophyllotoxin

Cat.No: T3S0027

Synonym: AXL 1717,Picropodophyllin,苦鬼臼毒素

Target: IGF-1R

2,3,4,6,8-Pentahydroxy-1-methylxanthone

Cat.No: T83411

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