Cat. No. | Product Name | Target | Signaling Pathways |
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T61730 |
Tyrosine kinase-IN-4
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Tyrosine kinase-IN-4 (EXAMPLE 107) 是一种酪氨酸激酶 (tyrosine kinase) 抑制剂。 | |||
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)。 | |||
T7568 |
LM22A-4
|
Trk receptor | Tyrosine Kinase/Adaptors |
LM22A-4 是特异性的tyrosine kinase receptor B 激动剂,常用于研究神经系统疾病。 | |||
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。 | |||
T4235 |
Roblitinib
FGF-401 |
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Roblitinib (FGF-401) 是一种口服有效的,高选择性的FGFR4抑制剂(IC50:1.9 nM),具有抗癌作用。 | |||
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。 | |||
T3550 |
X-376
Ensartinib,X-396,恩沙替尼 |
c-Met/HGFR; ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
X-376 (Ensartinib) 是一种有效的ALK 抑制剂,对许多具有crizotinib 抗性的ALK 突变型和中枢神经系统转移具有高活性。它能有效地抑制野生型ALK 和ALK 变体(F1174, C1156Y, L1196M, S1206R, T1151和G1202R 突变型),IC50小于4 nM。 | |||
TP1895L1 |
KYL acetate(676657-00-4 free base)
|
Ephrin Receptor | Tyrosine Kinase/Adaptors |
KYL acetate(676657-00-4 free base) 是EphA4受体酪氨酸激酶抑制剂(Kd = 0.8 μM);抑制 EphA4-EphrinA5 相互作用 (IC50 = 6.34 μM)。防止 AβO 诱导的突触损伤、树突棘丢失并防止海马 CA3-CA1 传输中 LTP 的阻断。在细胞培养基中表现出较长的半衰期(在 PC3 和 C2C12 培养基中分别为 8 和 12 小时)。它有神经保护作用。 | |||
T36648 |
Tucatinib hemiethanolate
|
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Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ... | |||
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. | |||
T39919 |
A 410099.1, amine-Boc hydrochloride
|
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A 410099.1, amine-Boc hydrochloride, serves as a functionalized IAP (Inhibitor of Apoptosis Proteins) ligand instrumental in the synthesis of PROTACs (Proteolysis Targeting Chimeras), notably those targeting BTK (Bruton's Tyrosine Kinase), including PROTACs 4 and 5. | |||
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。 | |||
T37604 | ITK inhibitor | ||
Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminome... | |||
T67442 |
CGP-53716
|
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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... | |||
T62561 |
TRK-IN-17
|
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TRK-IN-17 是一种 TRK 的有效抑制剂。其中原肌球蛋白相关激酶 (Trks) 是受体酪氨酸激酶家族成员,由神经营养因子激活。神经营养因子是一组可溶性生长因子,包括神经生长因子 (NGF)、脑源性神经营养因子 (BDNF) 和神经营养因子-3 (NT-3),以及神经营养因子-4/5 (NT-4/5)。TRK-IN-17 具有潜力进行癌症疾病的研究。 | |||
T36102 |
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline
|
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4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline is a building block and synthetic intermediate.1,2,3,4,5It has been used as a precursor in the synthesis of receptor tyrosine kinase (RTK) inhibitors, dual RTK and histone deacetylase (HDAC) inhibitors, and anticancer compounds.1,2,3It is also a synthetic intermediate in the synthesis of EGFR inhibitors, including erlotinib , with antiproliferative activity.4,5 | |||
T82252 |
GTPγS tetralithium
|
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GTPγS (tetralithium) 是一种G蛋白激活剂,能够通过酪氨酸激酶依赖性机制刺激GLUT4的转位,并促进磷脂酶活化和肌动蛋白的聚合,从而可以作为蛋白质抑制蛋白酶介导降解的保护剂。此外,GTPγS (tetralithium) 在研究G蛋白α亚单位功能和激酶活性时可以与其结合使用,并可用作裂解缓冲液中的一个组分。 | |||
T36643 |
PKI-166 hydrochloride
|
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Potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable. Bruns et al (2000) Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 60 2926 PMID:10850439 |Ulu et al (2013) Epidermal ... |