Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4191 |
Multi-kinase inhibitor 1
Multi-kinase inhibitor I |
Others; Bcr-Abl; PDGFR; c-Kit | Angiogenesis; Cytoskeletal Signaling; Others; Tyrosine Kinase/Adaptors |
Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) 是多激酶抑制剂。它有用于导致与酪氨酸激酶活性异常或失控有关的疾病或失调的潜力,特别是与c-Kit,PDGF-R,Bcr-abl 活性相关的疾病。 | |||
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)。 | |||
T5093 |
Pim1/AKK1-IN-1
LKB1/AAK1 dual inhibitor,MDK-2275 |
Pim; Hippo pathway | Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) 是多种酶抑制剂,能够作用于Pim1、AKK1、MST2 和 LKB1,Kd 值分别为 35、53、75 和 380 nM,还抑制 MPSK1 和 TNIK。 | |||
T35570 |
Chiauranib
CS2164,西奥罗尼 |
c-Fms; VEGFR; FLT; PDGFR; c-Kit; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
Chiauranib 是一种针对肿瘤血管生成的多靶点抑制剂,具有强大的抗癌作用。 Chiauranib 有效抑制血管生成相关激酶(VEGFR1、VEGFR2、VEGFR3、PDGFRα 和 c-Kit)、有丝分裂相关激酶 Aurora B 和慢性炎症相关激酶 CSF1R,IC50 值范围为 1-9 nM。 | |||
T72604 |
Multi-kinase-IN-1
|
||
Multi-kinase-IN-1 是一种具有抗肿瘤活性的激酶 (kinase) 抑制剂。Multi-kinase-IN-1 诱导细胞凋亡 (apoptosis),可用于结直肠癌的研究。 | |||
T63967 |
Multi-kinase-IN-2
|
||
Multi-kinase-IN-2 是口服具有活力的血管激酶 (angiokinase) 抑制剂。Multi-kinase-IN-2 能够显著抑制血管激酶的活性,如 VEGFR-1/2/3、PDGFRα/β、FGFR-1、LYN 和 c-KIT 激酶。Multi-kinase-IN-2 能够明显减弱 AKT 和 ERK 蛋白的磷酸化,并可诱导细胞凋亡 (apoptosis),具有抗癌作用。 | |||
T69209 |
ZK-304709
|
||
ZK-304709 is a potent multi-target tumor growth inhibitor with IC50 = nanomolar inhibitory activity to cyclin-dependent kinases 1, 2, 4, 7 and 9, as well as vascular endothelial growth factor receptor tyrosine kinase 1-3 and of platelet-derived growth factor receptor beta tyrosine kinase. | |||
T13156 |
TG 100572
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
TG 100572 is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively). | |||
T13157L | TG 100801 Hydrochloride | VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
TG 100801 Hydrochloride is a prodrug to treat age-related macular degeneration. TG 100572 is a inhibitor of multi-targeted kinase(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, | |||
T9665 |
Esuberaprost Sodium
|
||
Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2]. | |||
T81740 | Multi-kinase-IN-6 | Trk receptor | Tyrosine Kinase/Adaptors |
Multi-kinase-IN-6 (compound 10e) 是一种效能极高的多激酶抑制剂,具有对 TrkA、ALK2、c-KIT、EGFR、PIM1、CK2α、CHK1 和 CDK2 等多种酶的显著抑制作用。在 MCF7、HCT116 和 EKVX 癌细胞系上,其抗增殖活性突出,IC50 值分别达到 3.36 μM、1.40 μM 与 3.49 μM。此外,Multi-kinase-IN-6 能引起 MCF7 与 HCT116 细胞的细胞周期在 G1/S 期及 G1 期停滞,并有效诱导凋亡。 | |||
T14282 |
Amuvatinib hydrochloride
HPK 56 hydrochloride,MP470 hydrochloride |
Others | Others |
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret and is also a DNA repair suppressor through suppression of DNA repai | |||
T61596 | EGFR/HER2/DHFR-IN-1 | ||
EGFR/HER2/DHFR-IN-1 is a highly selective and potent anticancer compound specifically targeting MCF-7 breast cancer cells. It acts as a multi-inhibitor, targeting the EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. Its mechanism of action involves cell cycle arrest at the G1/S phase and induction of apoptosis in cells [1]. | |||
T74021 | O-Demethyl Lenvatinib hydrochloride | ||
O-Demethyl Lenvatinib hydrochloride 是 Lenvatinib 的代谢物。Lenvatinib (E7080) 一种具有口服活性的,多靶点酪氨酸激酶抑制剂,VEGFR1-3、FGFR1-4、PDGFR、KIT 和 RET。Lenvatinib 显示有效抗癌的活性。 | |||
T13156L |
TG 100572 Hydrochloride
|
VEGFR; FGFR; PDGFR; Src | Angiogenesis; Tyrosine Kinase/Adaptors |
TG 100572 Hydrochloride 是一种多靶点激酶抑制剂,能够抑制受体酪氨酸激酶和Src 激酶。 | |||
T74020 |
O-Demethyl Lenvatinib
|
||
O-Demethyl Lenvatinib 是Lenvatinib 的代谢物。Lenvatinib (E7080) 一种具有口服活性的,多靶点酪氨酸激酶抑制剂,VEGFR1-3、FGFR1-4、PDGFR、KIT 和RET,显示有效抗癌的活性。 | |||
T61313 |
Antitumor agent-70
|
||
Antitumor agent-70 (compound 8b) is a highly potent multi-targeted kinase inhibitor, particularly targeting c-Kit. It demonstrates remarkable anti-tumor activity and the ability to induce cell apoptosis. This compound also exhibits strong inhibition of multiple myeloma, with an IC 50 value of 0.12 μM. Therefore, Antitumor agent-70 holds great potential as an effective therapy for combating cancer, especially in cases involving c-Kit. [1] | |||
T64090 | Regorafenib mesylate | ||
Regorafenib (BAY 73-4506) mesylate 是一种口服具有活力的多靶点受体酪氨酸激酶 (tyrosine kinase) 抑制剂,能够抑制VEGFR1/2/3 (IC50=13/4.2/46 nM),PDGFRβ (IC50: 22 nM),Kit (IC50: 7 nM),RET (IC50: 1.5 nM) 和 Raf-1 (IC50: 2.5 nM)。Regorafenib mesylate 具有强大的抗肿瘤和抗血管生成作用。 | |||
T78792 |
Multi-kinase-IN-4
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Multi-kinase-IN-4 (compound 5d) 是一种针对VEGFR2、EGFR、HER2和CDK2的多靶点激酶抑制剂,其IC50值依次为0.33、0.22、0.18和2.09 μM。该化合物对包括HepG2、MCF-7、MDA-231 和 HeLa 在内的多种细胞系展现出强效的抗癌活性,IC50值范围为1.94至7.1 µM,对WI-38细胞线则显示较低毒性,IC50值为40.85 µM。它能诱导HepG2细胞发生apoptosis并在S期阻滞细胞周期,适用于癌症相关的生物学研究。 | |||
T73196 |
RGB-286638
|
||
RGB-286638 是一种有效的 CDK 抑制剂,抑制cyclin T1-CDK9,cyclin B1-CDK1,cyclin E-CDK2,cyclin D1-CDK4,cyclin E-CDK3和p35-CDK5活性,IC50分别为 1,2,3,4,5 和 5 nM;同时可抑制GSK-3β,TAK1,Jak2和MEK1,IC50值分别为 3,5,50,和 54 nM。 |