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Cat. No. Product Name Target Signaling Pathways
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。
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。
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。
T4496 LM22B-10

LM22B10

ERK; Trk receptor; Akt Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
LM22B-10 是TrkB/TrkC 神经营养因子受体激活剂,诱导体内外TrkB、TrkC、AKT 和ERK 的活化。
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。
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。
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)。
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).
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).
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)。
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.
T71484 Utatrectinib

AZD-7451

Utatrectinib (AZD-7451) 是一种有效的、选择性的和具有口服活性的Trk 抑制剂。Utatrectinib 可阻断TrkC 激活和相关的致瘤行为。
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].
T61551 Trk-IN-20

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].
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].
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。
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。
T62076 LPM4870108

LPM4870108 是一种有效的、口服具有活力的泛 Trk (WT/MT) 抑制剂,能够作用于 TrkC (IC50: 0.2 nM)、TrkA (IC50: 2.4 nM)、TrkAG595R (IC50: 3.5 nM) 和 TrkAG667C (IC50: 2.3 nM),且对 Trk 的选择性高于 ALK (IC50: 182 nM)。LPM4870108 显示出抗肿瘤效果。
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。
T64070 Pan-Trk-IN-3

Pan-Trk-IN-3 是一种有效的广谱 Trk 及其耐药突变体抑制剂,能够作用于 TrkA (IC50: 2 nM)、TrkB (IC50: 3 nM)、TrkC (IC50: 2 nM)、TrkAG595R (IC50: 21 nM)、TrkAG667C (IC50: 26 nM)、TrkAG667S (IC50: 5 nM)、TrkAF589L (IC50: 7 nM) 和 TrkCG623R (IC50: 6 nM)。Pan-Trk-IN-3 能够诱导细胞凋亡 (apoptosis),具有显著的抗肿瘤效果。
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。
T72289 Type II TRK inhibitor 1

Trk receptor Tyrosine Kinase/Adaptors
Type II TRK inhibitor 1 是有效抑制多种TRK融合蛋白及野生型的TRK抑制剂。对携有CD74-TRKAG667C及ETV6-TRKCG696C融合蛋白的Ba/F3细胞表现出抗增殖活性,其IC50值分别为6 nM与1.7 nM。
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。
T22324 Ensartinib hydrochloride

Ensartinib dihydrochloride,X-396 dihydrochloride

Others; Trk receptor; c-Met/HGFR; ALK Angiogenesis; Others; Tyrosine Kinase/Adaptors
Ensartinib hydrochloride (X-396 dihydrochloride) 是双重的 ALK/MET 抑制剂,IC50分别 <0.4 nM 和 0.74 nM。
T2054 Altiratinib

DCC-2701

VEGFR; Tie-2; FLT; Trk receptor; c-Met/HGFR Angiogenesis; Tyrosine Kinase/Adaptors
Altiratinib (DCC-2701) 是一种多靶点激酶抑制剂,能够抑制 MET (IC50:2.7 nM),TIE2 (IC50:8 nM),VEGFR2 (IC50:9.2 nM),FLT3 (IC50:9.3 nM),Trk1 (IC50:0.85 nM),Trk2 (IC50:4.6 nM) 和 Trk3 (IC50:0.83 nM)。
T62788 Pexidartinib hydrochloride

Pexidartinib hydrochloride (PLX-3397 hydrochloride) 是一种有效的、选择性的、口服具有活力的、ATP-竞争性的集落刺激因子 1 (CSF1R 或 M-CSFR) (IC50: 20 nM) 和 c-Kit (IC50: 10 nM) 抑制剂。Pexidartinib hydrochloride 对 c-Kit 和 CSF1R 的选择性是对其他相关激酶的 10-100 倍,作用于 FLT3 (IC50: 160 nM)、KDR (VEGFR2) (IC50: 350 nM)、LCK (IC50: 860 nM)、FLT1 (VEGFR1) (IC50: 880 nM) 和 NTRK3 (TRKC) (IC50: 890 nM)。Pexidartinib hydrochloride 能够诱导细胞凋亡,表现出抗肿瘤作用。
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.

化合物

RIPK1-IN-7
Cat.No: T12731
Synonym:
Target: RIP kinase
Selitrectinib
Cat.No: T7435
Synonym: LOXO-195
Target: Trk receptor
CH7057288
Cat.No: T5635
Synonym:
Target: Trk receptor
Belizatinib
Cat.No: T4257
Synonym: TSR-011
Target: Trk receptor, ALK
LM22B-10
Cat.No: T4496
Synonym: LM22B10
Target: ERK, Trk receptor, Akt
Entrectinib
Cat.No: T3678
Synonym: RXDX-101,恩曲替尼,NMS-E628
Target: Trk receptor, ROS, ALK, Autophagy, ROS Kinase
CG 428
Cat.No: T41224
Synonym:
Target: Trk receptor
GNF-5837
Cat.No: T6097
Synonym: GNF 5837
Target: Trk receptor, PDGFR, c-Kit
Trk-IN-4
Cat.No: T17169
Synonym: PF-6683324 isomer
Target: Trk receptor
PF-06737007
Cat.No: T17170
Synonym:
Target: Trk receptor
TRK-IN-23
Cat.No: T78968
Synonym:
Target: Trk receptor
PF-06733804
Cat.No: T13207
Synonym:
Target: Trk receptor
Utatrectinib
Cat.No: T71484
Synonym: AZD-7451
Target:
Trk-IN-8
Cat.No: T61712
Synonym:
Target:
Trk-IN-20
Cat.No: T61551
Synonym:
Target:
Trk-IN-7
Cat.No: T61443
Synonym:
Target:
IHMT-TRK-284
Cat.No: T63076
Synonym:
Target:
Taletrectinib
Cat.No: T22318
Synonym: DS-6051b,AB-106
Target: Trk receptor, ROS, ROS Kinase
LPM4870108
Cat.No: T62076
Synonym:
Target:
TrkA-IN-3
Cat.No: T73306
Synonym:
Target:
Pan-Trk-IN-3
Cat.No: T64070
Synonym:
Target:
TRK II-IN-1
Cat.No: T73033
Synonym:
Target: Trk receptor
Type II TRK inhibitor 1
Cat.No: T72289
Synonym:
Target: Trk receptor
TRK-IN-24
Cat.No: T79706
Synonym:
Target: Trk receptor
Ensartinib hydrochloride
Cat.No: T22324
Synonym: Ensartinib dihydrochloride,X-396 dihydrochloride
Target: Others, Trk receptor, c-Met/HGFR, ALK
Altiratinib
Cat.No: T2054
Synonym: DCC-2701
Target: VEGFR, Tie-2, FLT, Trk receptor, c-Met/HGFR
Pexidartinib hydrochloride
Cat.No: T62788
Synonym:
Target:
TrkA-IN-1
Cat.No: T13208
Synonym:
Target: Trk receptor
TargetMol Loading
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