trk

Trk-IN-9 是一种 TRK 抑制剂，具有抗癌抗增殖活性，可以浓度依赖性方式诱导 Km-12 细胞凋亡。Trk-IN-9可用于研究癌症。

LOXO-195 (BAY 2731954) 是一种有效的选择性 Trk 酪氨酸激酶抑制剂。

GNF-8625 monopyridin-N-piperazine hydrochloride 是一种原肌球蛋白受体激酶（TRK） 的抑制剂。

Larotrectinib sulfate (LOXO-101 sulfate) 是一种 ATP 竞争性的，口服选择性抑制剂，对原肌凝蛋白相关激酶家族受体的三个亚型具有纳摩尔级别的 50% 抑制浓度。

Larotrectinib (LOXO-101)为ATP竞争性、口服选择性抑制剂，针对原肌凝蛋白相关激酶(TRK)家族受体三个亚型(TRKA，B 和C)展现纳摩尔级别的50%抑制浓度。

Selitrectinib (LOXO-195) 是异种选择性的二代原肌凝蛋白相关激酶(TRK)抑制剂，能够作用于 TRKA (IC50:0.6 nM) 和 TRKC (IC50<2.5 nM)。

Thalidomide-5-NH2-CH2-COOH (compound 114) 是原肌球蛋白受体激酶的选择性抑制剂。它是 E3 连接酶的配体，具有研究一种或多种疾病的潜力。

CH7057288 是选择性TRK 抑制剂。

Tyrphostin AG 879 (AG 879) 是一种抑制TrKA 磷酸化的酪氨酸激酶抑制剂，IC50为 10 μM。它还是一种选择性ErbB2酪氨酸激酶抑制剂，IC50为 1 μM，具有抗癌活性。

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。

DDR-TRK-1 是 DDR1的一个选择性抑制剂，其 IC50 值为 9.4 nM。DDR-TRK-1 也抑制 TRK 激酶家族。

Trk-IN-4 (PF-6683324)是一种有效的泛-Trk抑制剂，对TrkA TrkB TrkC的IC50 = 1.1~2.6 nM，具有抗痛觉过敏作用。也是选择性的II型PTK6抑制剂，IC50=76nM，具有抗肿瘤作用。

IHMT-TRK-284 (Compound 34) 是一种有效的、口服具有活力的 type II TRK kinase 抑制剂，能够作用于 TRKA (IC50: 10.5 nM)、TRKB (IC50: 0.7 nM)、TRKC (IC50: 2.6 nM)。IHMT-TRK-284 在激酶组中表现出良好的选择性，体内具有良好的抗肿瘤作用。

TRK-IN-30 (Compound C11) 是一种原肌球蛋白受体激酶（TRK）抑制剂，针对TRKA、TRKB、TRKC和耐药突变体TRKAG595R的IC50分别为1.8、0.98、3.8和54 nM。该化合物能够抑制下游PI3K AKT和MEK ERK信号通路的激活，并且对Km-12细胞系具有显著作用，抑制其菌落形成和细胞迁移，造成细胞周期在G0 G1期停滞，并诱导Km-12细胞凋亡 (apoptosis)。

DDR-TRK-1N is a negative control for DDR-TRK-1.

TRK-IN-15 (WO2012034091A1, compound X-55) is a highly effective inhibitor of TRK, a protein kinase with crucial involvement in the regulation of cellular growth, differentiation, and signal transduction. Offering significant potential for studying TRK-related diseases, TRK-IN-15 holds promise for advancing research in this field [1].

TRK-IN-16 (WO2012034091A1, compound X-21) is a highly effective TRK inhibitor, targeting protein kinases that are integral to regulating cell growth, differentiation, and various cellular signal transduction processes. This compound shows great potential for research in TRK-related diseases [1].

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].

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].

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].

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].

Trk-IN-11 (Compound 14h) 是一种 TRK 的有效抑制剂，对 TrkA、TrkA G595R 的 IC50 值分别为 1.4 nM、1.8 nM。其中原肌球蛋白受体激酶 (Trk) 是一种受体酪氨酸激酶 (RTK)，也是实体瘤中关键的药物靶点。Trk-IN-11对癌症疾病表现出研究潜力。

TRK-IN-19 (Compound I-10 ) 是一种 TRK 的有效抑制剂，对 TRKA、TRKAG595R 的 IC50 值分别为 1.1 nM、5.3 nM。TRK-IN-19 对癌症疾病表现出潜在的研究价值。

TRK-IN-21 (5n) 是一种口服具有活力的 TRK 抑制剂。TRK-IN-21 能够作用于 TRKAWT (IC50: 0.3 nM)，TRKAG667C (IC50: 2.3 nM)，TRKAF589L (IC50: 0.4 nM)和 TRKAG595 (IC50: 0.5 nM)。TRK-IN-21 能够用于研究癌症。