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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.
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。
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。
T73306 TrkA-IN-3

TrkA-IN-3 是一种有效和亚选择性的TrkA 变构抑制剂,IC50值为 22.4 nM。TrkA-IN-3 对TrkA 的选择性超过TrkB 和TrkC8000 倍。TrkA-IN-3 可用于研究疼痛。
T16766 Ro 08-2750

Ro 08-2750 是一种非肽和可逆的神经生长因子 (NGF) 抑制剂,与 NGF 结合,IC50 约为 1 µM。它是一种选择性 MSI RNA 结合活性抑制剂,IC50 为 2.7 μM。它选择性抑制 NGF 与 p75NTR 的结合,而不是 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。
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。
T6712 Tyrphostin AG 879

AG 879

Apoptosis; EGFR; Trk receptor; HER; PDGFR Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
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。
T4349 Sitravatinib

MG516,MGCD516

Discoidin Domain Receptor (DDR); VEGFR; FLT; Trk receptor; TAM Receptor; c-Kit; Ephrin Receptor Angiogenesis; Tyrosine Kinase/Adaptors
Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效,且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。
T0678 Amitriptyline hydrochloride

Amitriptyline HCl,Tryptizol,盐酸阿米替林,Domical,Annoyltin

Trk receptor; Sigma receptor; 5-HT Receptor; Serotonin Transporter; Sodium Channel; Adrenergic Receptor; AChR; Norepinephrine; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; Tyrosine Kinase/Adaptors
Amitriptyline hydrochloride (Annoyltin) 是血清素再摄取转运体和去甲肾上腺素再摄取转运体抑制剂,还与多巴胺再摄取转运体结合,其Ki 为 2.58 μM。它也抑制肾上腺素能受体、毒蕈碱受体、组胺受体、5-羟色胺受体。它是TrkATrkA 受体的激动剂,具有强神经营养活性和有抗抑郁作用。
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.
T63223 hTrkA-IN-2

hTrkA-IN-2 是选择性的 hTrkA 变构抑制剂(IC50: 3.9 nM)。
T7435 Selitrectinib

LOXO-195

Trk receptor Tyrosine Kinase/Adaptors
Selitrectinib (LOXO-195) 是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)。
T5635 CH7057288

Trk receptor Tyrosine Kinase/Adaptors
CH7057288 是选择性TRK 抑制剂。
T14921 CE-245677

Tie-2; Trk receptor Tyrosine Kinase/Adaptors
CE-245677 是可逆的Tie2和TrkA/B 抑制剂,在细胞体系下的IC50值分别为 4.7 和 1 nM。
T14363 AZ-23

AZ 23,AZ23

Trk receptor Tyrosine Kinase/Adaptors
AZ-23是一种 ATP-竞争性的,口服具有活性的 Trk 激酶 A/B/C 抑制剂,IC50值分别为2 nM (TrkA),8 nM (TrkB),24 nM (FGFR1),52 nM (Flt3),55 nM (Ret),84 nM (MuSk),99 nM (Lck)。
T6097 GNF-5837

GNF 5837

Trk receptor; PDGFR; c-Kit Angiogenesis; Tyrosine Kinase/Adaptors
GNF-5837 是一种选择性的,有效的,口服生物利用的泛TRK 抑制剂,在 Ba/F3 细胞中显示出抗增殖作用 (对Tel-TrkC,Tel-TrkB 和Tel-TrkA 的IC50值分别为 7 nM,9 nM 和 11 nM)。
T9292 ALE-0540

ALE0540

Others; Trk receptor Others; Tyrosine Kinase/Adaptors
ALE-0540是一种非肽类杂环分子,可抑制NGF 与p75和TrkA 的结合,以及TrkA 受体介导的信号转导和生物反应。
T6052 GW 441756

Apoptosis; Raf; Trk receptor; CDK Apoptosis; Cell Cycle/Checkpoint; MAPK; Tyrosine Kinase/Adaptors
GW 441756 是一种高特异性神经生长因子受体酪氨酸激酶 a 抑制剂 ,IC50值为 2 nM,可消除 BmK NSPK 诱导神经突生长。
T4257 Belizatinib

TSR-011

Trk receptor; ALK Angiogenesis; Tyrosine Kinase/Adaptors
Belizatinib (TSR-011) 是可口服的ALK 和 TRKA、TRKB、TRKC 双重抑制剂,对野生型重组 ALK 的IC50值为0.7 nM。
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。
T62447 Paltimatrectinib

PBI-200,PPI-5278

Trk receptor; Tyrosine Kinases Tyrosine Kinase/Adaptors
Paltimatrectinib (PBI-200) 是一种高效的酪氨酸激酶 (tyrosine kinase) 抑制剂,具有抗癌活性,抑制肌球蛋白相关激酶 A (TrkA) 。Paltimatrectinib 可用于研究膀胱癌、乳腺癌和结直肠癌。
T41224 CG 428

Trk receptor Tyrosine Kinase/Adaptors
CG 428 是一种有效的原肌球蛋白受体激酶 (TRK) 降解剂 (uSMITETM),DC50 为 0.36 nM。 CG 428 包含泛 TRK 抑制剂 GNF-8625 的类似物,通过接头连接到 cereblon E3 连接酶配体泊马度胺。 CG 428 对 TRKA 的选择性优于 TRKC 和 TRKB,Kd 为 1nM、4.2 nM 和 28 nM。 CG 428 抑制 KM12 结肠癌细胞的生长,IC50 为 2.9 nM。
T2349 BMS-754807

Trk receptor; c-Met/HGFR; IGF-1R Tyrosine Kinase/Adaptors
BMS754807 是一种可逆的IGF-1R 抑制剂 (IC50:1.8 nM,Ki<2 nM),也是一种可逆的IR 抑制剂 (IC50:7 nM,Ki<2 nM)。它也抑制 Met (IC50:6 nM),RON (IC50:44 nM),TrkA (IC50:7 nM),TrkB (IC50:4 nM),AurA (IC50:9 nM) 和 AurB (IC50:25 nM) 的活性。
T4071 Repotrectinib

TPX-0005,TPX 0005,TPX0005

Trk receptor; ROS; Src; ALK; ROS Kinase Angiogenesis; Immunology/Inflammation; Tyrosine Kinase/Adaptors
Repotrectinib (TPX-0005) 是ROS1(IC50=0.07 nM) 和TRK(对 TRKA/B/C 的IC50=0.83/0.05/0.1 nM) 抑制剂,能够抑制 WTALK(IC50=1.01 nM)。它具有抗癌作用。
T5995 Larotrectinib

LOXO-101,ARRY-470

Apoptosis; Trk receptor Apoptosis; Tyrosine Kinase/Adaptors
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。
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)。
T17169 Trk-IN-4

PF-6683324 isomer

Trk receptor Tyrosine Kinase/Adaptors
Trk-IN-4 is an effective pan-Trk inhibitor in cell-based assays (IC50s: 1.9 nM, 2.6 nM, and 1.1 nM for TrkA, TrkB, and TrkC, respectively).
T11729 JTE-952

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
JTE-952 is a oral, potent active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse
T13207 PF-06733804

Trk receptor Tyrosine Kinase/Adaptors
PF-06733804 is a potent inhibitor of pan-Trk in cell-based assays (IC50s: 8.4 nM, 6.2 nM, and 2.2 nM for TrkA, TrkB, and TrkC) with anti-hyperalgesic effect.
T15738 Lestaurtinib

KT-5555,CEP-701

Others Others
Lestaurtinib is a multi-kinase inhibitor. It also has effective activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3, and TrkA (IC50s: 0.9, 3, and less than 25 nM).
T17000 Tavilermide

MIM-D3

Trk receptor Tyrosine Kinase/Adaptors
Tavilermide is a selective and partial agonist of TrkA or a nerve growth factor mimetic.
T62672 D5261

D5261 是一个有效的、类型 III 变构的 tropomyosin-related kinase A (TrkA) 抑制剂。
T29020 TSR-011-isomer

TSR011 isomer,TSR-011 isomer,Belizatinib isomer

TSR011-isomer, a TrKA/ALK inhibitor, is used potentially for the treatment of solid tumours and lymphoma.
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。
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。
T17170 PF-06737007

Trk receptor Tyrosine Kinase/Adaptors
PF-06737007 is an effective inhibitor of pan-Trk in cell-based assays (IC50s: 7.7 nM, 15 nM, and 3.9 nM for TrkA, TrkB, and TrkC, respectively).
T22318 Taletrectinib

DS-6051b,AB-106

Trk receptor; ROS; ROS Kinase Immunology/Inflammation; Tyrosine Kinase/Adaptors
Taletrectinib (AB-106) 是具有口服活力的、选择性的 ROS1/NTRK 抑制剂。它对重组 ROS1、NTRK1、NTRK2 和 NTRK3 有较强的抑制作用,IC50值分别为 0.207、0.622、2.28 和 0.98 nM。它还抑制 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变体。
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].
T62341 (R)-Larotrectinib

(R)-Larotrectinib 是一种 TRK 的有效抑制剂,作用于 TrkA (IC50: 28.5 nM)。(R)-Larotrectinib 能够用于研究癌症、炎症以及某些感染性疾病。
T12925 Sitravatinib malate

MGCD516 malate,MG-516 malate

TAM Receptor Tyrosine Kinase/Adaptors
Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
T71121 Milciclib maleate

Milciclib maleate is an inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA).
T62093 Trk-IN-11

Trk-IN-11 (Compound 14h) 是一种 TRK 的有效抑制剂,对 TrkATrkA 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。
T62095 TRK-IN-19

TRK-IN-19 (Compound I-10 ) 是一种 TRK 的有效抑制剂,对 TRKATRKAG595R 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。
T39896 ALK-IN-9

ALK-IN-9 (compound 40) is a highly effective ALK inhibitor. It demonstrates remarkable inhibitory activity against cell proliferation, with IC50 values of <0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), and KG-l cell (OP2-FGFR1).
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].
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。
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。
T63076 IHMT-TRK-284

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。

化合物

TrkA-IN-1
Cat.No: T13208
Synonym:
Target: Trk receptor
ITK/TRKA-IN-1
Cat.No: T40294
Synonym:
Target:
TrkA-IN-4
Cat.No: T73307
Synonym:
Target:
FLT3/TrKA-IN-1
Cat.No: T62801
Synonym:
Target:
TrkA-IN-3
Cat.No: T73306
Synonym:
Target:
Ro 08-2750
Cat.No: T16766
Synonym:
Target:
RIPK1-IN-7
Cat.No: T12731
Synonym:
Target: RIP kinase
DS-1205
Cat.No: T9123
Synonym:
Target: TAM Receptor
Tyrphostin AG 879
Cat.No: T6712
Synonym: AG 879
Target: Apoptosis, EGFR, Trk receptor, HER, PDGFR
Sitravatinib
Cat.No: T4349
Synonym: MG516,MGCD516
Target: Discoidin Domain Receptor (DDR), VEGFR, FLT, Trk receptor, TAM Receptor, c-Kit, Ephrin Receptor
Amitriptyline hydrochloride
Cat.No: T0678
Synonym: Amitriptyline HCl,Tryptizol,盐酸阿米替林,Domical,Annoyltin
Target: Trk receptor, Sigma receptor, 5-HT Receptor, Serotonin Transporter, Sodium Channel, Adrenergic Receptor, AChR, Norepinephrine, Histamine Receptor
hTrkA-IN-1
Cat.No: T39266
Synonym:
Target:
hTrkA-IN-2
Cat.No: T63223
Synonym:
Target:
Selitrectinib
Cat.No: T7435
Synonym: LOXO-195
Target: Trk receptor
CH7057288
Cat.No: T5635
Synonym:
Target: Trk receptor
CE-245677
Cat.No: T14921
Synonym:
Target: Tie-2, Trk receptor
AZ-23
Cat.No: T14363
Synonym: AZ 23,AZ23
Target: Trk receptor
GNF-5837
Cat.No: T6097
Synonym: GNF 5837
Target: Trk receptor, PDGFR, c-Kit
ALE-0540
Cat.No: T9292
Synonym: ALE0540
Target: Others, Trk receptor
GW 441756
Cat.No: T6052
Synonym:
Target: Apoptosis, Raf, Trk receptor, CDK
Belizatinib
Cat.No: T4257
Synonym: TSR-011
Target: Trk receptor, ALK
Entrectinib
Cat.No: T3678
Synonym: RXDX-101,恩曲替尼,NMS-E628
Target: Trk receptor, ROS, ALK, Autophagy, ROS Kinase
Paltimatrectinib
Cat.No: T62447
Synonym: PBI-200,PPI-5278
Target: Trk receptor, Tyrosine Kinases
CG 428
Cat.No: T41224
Synonym:
Target: Trk receptor
BMS-754807
Cat.No: T2349
Synonym:
Target: Trk receptor, c-Met/HGFR, IGF-1R
Repotrectinib
Cat.No: T4071
Synonym: TPX-0005,TPX 0005,TPX0005
Target: Trk receptor, ROS, Src, ALK, ROS Kinase
Larotrectinib
Cat.No: T5995
Synonym: LOXO-101,ARRY-470
Target: Apoptosis, Trk receptor
TRK-IN-23
Cat.No: T78968
Synonym:
Target: Trk receptor
Trk-IN-4
Cat.No: T17169
Synonym: PF-6683324 isomer
Target: Trk receptor
JTE-952
Cat.No: T11729
Synonym:
Target: Histamine Receptor
PF-06733804
Cat.No: T13207
Synonym:
Target: Trk receptor
Lestaurtinib
Cat.No: T15738
Synonym: KT-5555,CEP-701
Target: Others
Tavilermide
Cat.No: T17000
Synonym: MIM-D3
Target: Trk receptor
D5261
Cat.No: T62672
Synonym:
Target:
TSR-011-isomer
Cat.No: T29020
Synonym: TSR011 isomer,TSR-011 isomer,Belizatinib isomer
Target:
TRK II-IN-1
Cat.No: T73033
Synonym:
Target: Trk receptor
TRK-IN-24
Cat.No: T79706
Synonym:
Target: Trk receptor
PF-06737007
Cat.No: T17170
Synonym:
Target: Trk receptor
Taletrectinib
Cat.No: T22318
Synonym: DS-6051b,AB-106
Target: Trk receptor, ROS, ROS Kinase
Trk-IN-10
Cat.No: T61872
Synonym:
Target:
(R)-Larotrectinib
Cat.No: T62341
Synonym:
Target:
Sitravatinib malate
Cat.No: T12925
Synonym: MGCD516 malate,MG-516 malate
Target: TAM Receptor
Milciclib maleate
Cat.No: T71121
Synonym:
Target:
Trk-IN-11
Cat.No: T62093
Synonym:
Target:
TRK-IN-19
Cat.No: T62095
Synonym:
Target:
ALK-IN-9
Cat.No: T39896
Synonym:
Target:
Trk-IN-7
Cat.No: T61443
Synonym:
Target:
TRAF6 peptide TFA
Cat.No: T78221
Synonym:
Target: E1/E2/E3 Enzyme
Bedinvetmab
Cat.No: T76813
Synonym:
Target:
IHMT-TRK-284
Cat.No: T63076
Synonym:
Target:
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