Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13208 |
TrkA-IN-1
|
Trk receptor | Tyrosine Kinase/Adaptors |
TrkA-IN-1 is a potent and selective inhibitor of Tropomyosin-related kinase A (TrkA) (IC50: 99 nM in a cell-based assay) with analgesic activity. | |||
T40294 |
ITK/TRKA-IN-1
|
||
ITK/TRKA-IN-1 is a chemical compound that functions as a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA). With an IC50 value of 1.0 nM, it effectively inhibits the activity of ITK, while demonstrating a remarkable 96% inhibition of TRKA. | |||
T12731 |
RIPK1-IN-7
|
RIP kinase | Apoptosis; NF-κB |
RIPK1-IN-7 是一种选择性有效的 RIPK1 抑制剂,Kd 值为 4 nM,IC50值为 11 nM。在实验性 B16 黑色素瘤肺转移模型中表现出优异的抗转移活性。 | |||
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。 | |||
T9123 |
DS-1205
|
TAM Receptor | Tyrosine Kinase/Adaptors |
DS-1205b free base 是有效的AXL 激酶选择性抑制剂,IC50为 1.3 nM。它对MER,MET 和TRKA 也有抑制作用,IC50分别为 63、104 和 407 nM。 它可以抑制细胞迁移和肿瘤生长。 | |||
T3678 |
Entrectinib
RXDX-101,恩曲替尼,NMS-E628 |
Trk receptor; ROS; ALK; Autophagy; ROS Kinase | Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Entrectinib (RXDX-101) 是一种可口服的 Trk、ROS1和 ALK 抑制剂,具有抗肿瘤和中枢神经活性,抑制 TrkA、TrkB、TrkC、ROS1 和 ALK 的 IC50值分别为 1、3、5、12 和 7 nM。 | |||
T73307 | TrkA-IN-4 | ||
TrkA-IN-4 是一种有效和具有口服活性的 TrkA 变构抑制剂,是TrkA-IN-3 的前药。TrkA-IN-4 显示出有效的抗伤害作用。 | |||
T78968 | TRK-IN-23 | Trk receptor | Tyrosine Kinase/Adaptors |
TRK-IN-23 (compound 24b) 是一款口服活性TRK抑制剂,对TRKA、TRKC、TRKAG595R、TRKAF589L和TRKAG667C 表现出高效的抑制作用,其IC50值分别为0.5 nM、9 nM、14 nM、4.4 nM和4.8 nM。此外,TRK-IN-23 能够诱导含有TRKAG595R和TRKAG667C突变的Ba/F3细胞系进行细胞凋亡(apoptosis)。 | |||
T61872 |
Trk-IN-10
|
||
Trk-IN-10 (Compound 14j) is a highly effective inhibitor of TRK, with an IC50 of 0.86 nM against TrkA and 6.92 nM against TrkA G595R. As an RTK, Trk plays a crucial role as a drug target in solid tumors. Trk-IN-10 (IC50 = 350 nM against ALK) demonstrates superior selectivity in inhibiting Trk, which has potential implications for toxicity reduction [1]. | |||
T39266 |
hTrkA-IN-1
|
||
hTrkA-IN-1 is a potent and orally active inhibitor of TrkA kinase with an IC 50 of 1.3 nM, compound 2.hTrkA-IN-1 can be used for the study of inflammatory disease, such as prostatitis, pelvic, et al. | |||
T79706 |
TRK-IN-24
|
Trk receptor | Tyrosine Kinase/Adaptors |
TRK-IN-24(compound 10g)是一种针对Trk Receptor的抑制剂,它对TRKA、TRKC、TRKAG595R、TRKAG667C和TRKAF589L的抑制作用的IC50值分别达到5.21、4.51、6.77、1.42和6.13 nM。该化合物在BaF3-CD74-NTRK1G595R和BaF3-CD74-NTRK1G667C异种移植模型中显示出明显的抗肿瘤活性。此外,TRK-IN-24 能有效抑制携带SF、GK、xDFG等单点突变的Ba/F3细胞增殖,其IC50范围为1.43至47.56 nM。 | |||
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。 | |||
T61443 | Trk-IN-7 | ||
Trk-IN-7 (compound I-6) is a highly potent inhibitor of TRK, exhibiting IC50 values ranging from 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. In addition, Trk-IN-7 demonstrates notable inhibition against EML4-ALK (IC50 <15 nM), as well as ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC50 = 5-50 nM) [1]. | |||
T61712 | Trk-IN-8 | ||
Trk-IN-8, a powerful TRK inhibitor, demonstrates excellent potency against TRKAa, TRKA(G595R), and TRKC(G623R) with IC50 values of 0.42 nM, 0.89 nM, and 1.5 nM, respectively (WO2021115401A1, compound 3) [1]. | |||
T76813 | Bedinvetmab | ||
Bedinvetmab (ZTS-00508841)为针对神经生长因子(NGF)的犬单克隆抗体(mAb),通过抑制NGF与肌球蛋白原受体激酶A(trkA)及p75神经营养蛋白受体(p75NTR)的相互作用,应用于犬骨关节炎疼痛的研究。 | |||
T61551 |
Trk-IN-20
|
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Trk-IN-20 is a 3-vinylindazole derivative compound that effectively inhibits the functions of Trk kinases. It accomplishes this by suppressing the phosphorylation of TrkA, TrkB, and TrkC, with IC50 values of 1.6 nM, 2.9 nM, and 2.0 nM, respectively [1]. | |||
T68286 |
CE-245677 mesylate
|
||
CE-245677 is a selective, orally active Tie2 kinase inhibitor identified by Pfizer previously in development for the treatment of certain cancers. CE-245,677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50 of 4.7 and 1 nM, resp., displays >100x selectivity against a number of other angiogenic receptor tyrosine kinases (e.g. KDR, PDGFR, FGFR) and gene family panels, and demonstrates good oral absorption in in vivo rat PK studies (F=80%). | |||
T78221 |
TRAF6 peptide TFA
|
E1/E2/E3 Enzyme | Ubiquitination |
TRAF6 peptide TFA是一种抑制TRAF6-p62相互作用的特异性分子,可抑制NGF依赖的TrkA泛素化,展现在阿尔茨海默症(AD)、帕金森病、ALS、创伤性脑损伤、癫痫和中风等神经系统疾病研究中的应用潜力。 | |||
T72931 | TRK/ALK-IN-1 | ||
TRK/ALK-IN-1 是一种有效的 TRK 和 ALK 双重抑制剂。TRK/ALK-IN-1 在酶促测定中与抗增殖活性非常吻合,对 TRKA、ALKIC50值分别为 2.2、9.3 和 38 nM< sup>WT 和 ALKL1196M。TRK/ALK-IN-1具有研究癌症疾病的潜力。 | |||
T78282 |
Tanezumab
RN-624,PF 4383119 |
||
Tanezumab (RN-624) 是一种针对神经生长因子(NGF)的人源化单克隆抗体,具有高度的亲和力和特异性,它通过阻断NGF与p75和TrkA受体的结合来发挥作用,这些受体存在于周围神经系统中。Tanezumab 主要用于研究治疗各种急性及慢性疼痛症状,包括骨关节炎、膝关节炎、神经痛以及带状疱疹后神经痛。 | |||
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。 | |||
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... |