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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。
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。
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)。
T5635 CH7057288

Trk receptor Tyrosine Kinase/Adaptors
CH7057288 是选择性TRK 抑制剂。
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)。
T4257 Belizatinib

TSR-011

Trk receptor; ALK Angiogenesis; Tyrosine Kinase/Adaptors
Belizatinib (TSR-011) 是可口服的ALK 和 TRKATRKB、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 TrkATrkB、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。
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。
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).
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.
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).
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.
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。
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].
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。
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].
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。
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。
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。
T37582 Ganglioside GM1 Mixture (ovine) (ammonium salt)

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...
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
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
GNF-5837
Cat.No: T6097
Synonym: GNF 5837
Target: Trk receptor, PDGFR, c-Kit
CH7057288
Cat.No: T5635
Synonym:
Target: Trk receptor
AZ-23
Cat.No: T14363
Synonym: AZ 23,AZ23
Target: Trk receptor
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
CG 428
Cat.No: T41224
Synonym:
Target: Trk receptor
BMS-754807
Cat.No: T2349
Synonym:
Target: Trk receptor, c-Met/HGFR, IGF-1R
Trk-IN-4
Cat.No: T17169
Synonym: PF-6683324 isomer
Target: Trk receptor
PF-06733804
Cat.No: T13207
Synonym:
Target: Trk receptor
PF-06737007
Cat.No: T17170
Synonym:
Target: Trk receptor
Sitravatinib malate
Cat.No: T12925
Synonym: MGCD516 malate,MG-516 malate
Target: TAM Receptor
TrkA-IN-3
Cat.No: T73306
Synonym:
Target:
Trk-IN-7
Cat.No: T61443
Synonym:
Target:
TRK II-IN-1
Cat.No: T73033
Synonym:
Target: Trk receptor
Trk-IN-20
Cat.No: T61551
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
CE-245677
Cat.No: T14921
Synonym:
Target: Tie-2, Trk receptor
Pan-Trk-IN-3
Cat.No: T64070
Synonym:
Target:
Ganglioside GM1 Mixture (ovine) (ammonium salt)
Cat.No: T37582
Synonym:
Target:
TrkA-IN-1
Cat.No: T13208
Synonym:
Target: Trk receptor
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