Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8467 |
RET V804M-IN-1
RETV804M kinase inhibitor,LUN09945 |
c-RET | Apoptosis; Tyrosine Kinase/Adaptors |
RET V804M-IN-1 (RETV804M kinase inhibitor) 是一种 wt-RET 选择性的RETV804M 激酶抑制剂,其IC50=20 nM。 | |||
T16735 |
RET-IN-1
|
Others | Others |
RET-IN-1 is a RET kinase inhibitor (IC50s: 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively). | |||
T78683 | RET-IN-22 | ||
RET-IN-22(compound 17b)是一种有效且选择性的口服活性RET抑制剂,其对野生型RET和RET-V804M的IC50分别为20.9 nM与18.3 nM。该化合物展现出对多数激酶,特别是EGFR和VEGFR2的高度选择性,表现出抗癌活性。 | |||
T64103 |
RET-IN-12
|
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RET-IN-12 是一种 RET 抑制剂,能够作用于 RET(WT) (IC50: 0.3 nM) 和 RET(V804M) (IC50: 1 nM)。 | |||
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。 | |||
T81296 |
RET-IN-26
|
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RET-IN-26(化合物D5)是一种RET kinase抑制剂,其IC50值为0.33 μM。 | |||
T79099 | RET-IN-23 | ||
RET-IN-23(化合物17)是一种有效的口服RET抑制剂,其IC50值对应RET-WT为1.32 nM、RET-CCDC6为2.50 nM、RET-V804L为6.54 nM、RET-V804M为1.03 nM及RET-M918T为1.47 nM。该化合物展现出了明显的抗肿瘤活性。 | |||
T77646 |
Multi-kinase-IN-5
|
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Multi-kinase-IN-5 (compound 15c) 是一种抑制广泛蛋白激酶的有效化合物,能够针对RET、KIT、cMet、VEGFR1、VEGFR2、FGFR1、PDGFR和BRAF展现出74%、31%、62%、40%、73%、74%、59%和69%的抑制效果。具体而言,其对FGFR1、VEGFR和RET激酶的IC50分别为1.287、0.117和1.185μM。 | |||
T79726 |
RET-IN-25
|
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RET-IN-25(化合物6b)是一种具有抗癌活性的RET激酶抑制剂。该化合物能够抑制甲状腺髓样癌(MTC),在TT(C634R) MTC细胞系中的IC50值分别为3.6 μM(3天)和3.0 μM(6天)。 | |||
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 | |||
T78203 |
NSC194598
|
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NSC194598是一种p53 DNA结合抑制剂,其体外和体内抑制p53序列特异性DNA结合的IC50值分别约为180 nM和2-40 μM。在人甲状腺髓样癌TT细胞中,NSC194598能够干扰突变RET基因的转录激活。该化合物可应用于研究放射及化学疗法对正常组织造成的急性毒性。 | |||
T78871 |
PLM-101
|
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PLM-101是一种口服抗癌剂,针对FLT3和RET具有选择性抑制作用,有效抑制急性髓系白血病(AML)细胞。通过抑制RET,PLM-101促使FLT3的自噬降解,并且通过抑制PI3K和Ras/ERK信号通路来发挥其抗白血病的活性。在小鼠MV4-11侧翼异种移植模型中,PLM-101以口服剂量3及10 mg/kg显示出抗肿瘤效果,并且在同种异种移植小鼠模型中,剂量为40 mg/kg(口服)亦展现出明显的抗肿瘤功效。 | |||
T73033 | TRK II-IN-1 | Trk receptor | Tyrosine Kinase/Adaptors |
TRKII-IN-1 是一种有效的 II 型TRK抑制剂,对TRKA/B/C及TRKAG667C的IC50分别为3.3、6.4、4.3 和 9.4 nM。此外,TRKII-IN-1 对FLT3、RET和VEGFR2也具有抑制作用,其IC50分别为1.3、9.9 和 71.1 nM。TRKII-IN-1 主要用于TRK驱动的癌症研究。 | |||
T37582 |
Ganglioside GM1 Mixture (ovine) (ammonium salt)
|
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Ganglioside GM1is a monosialylated ganglioside and the prototypic ganglioside for those containing one sialic acid residue.1,2It is found in a large variety of cells, including immune cells and neurons, and is enriched in lipid rafts in the cell membrane.3It associates with growth factor receptors, including TrkA, TrkB, and the GDNF receptor complex containing Ret and GFRα, and is required for TrkA expression on the cell surface. Ganglioside GM1interacts with other proteins to increase calcium i... |