Search Result
Results for "
Trk inhibitors
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-N0020
-
|
|
Wnt
Reactive Oxygen Species (ROS)
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Neurological Disease
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Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche deserticola, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity .
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-
-
- HY-12866
-
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LOXO-101; ARRY-470
|
Trk Receptor
Apoptosis
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Cancer
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Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
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-
-
- HY-103022
-
-
-
- HY-N6732
-
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SF2370; Antibiotic K 252a; Antibiotic SF 2370
|
Autophagy
PKA
PKC
Trk Receptor
CaMK
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Infection
Inflammation/Immunology
|
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K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively . K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene .
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-
-
- HY-13491
-
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Trk Receptor
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Cancer
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GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
|
-
-
- HY-101977
-
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LOXO-195
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Trk Receptor
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Cancer
|
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Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC50s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively .
|
-
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- HY-152292
-
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NVL-520; NUV-520
|
ROS Kinase
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Cancer
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Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer .
|
-
-
- HY-10424
-
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PHA-848125
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CDK
Autophagy
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Cancer
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Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
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-
-
- HY-148811
-
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ICP-723
|
c-Met/HGFR
Trk Receptor
|
Cancer
|
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Zurletrectinib is a brain-penetrant, orally active TRK inhibitor (TRKA IC50 = 0.81 nM; TRKB IC50 = 0.145 nM; TRKC IC50 = 0.184 nM). Zurletrectinib exhibits stronger activity as a consequence of its augmented binding affinity for TRK kinases. Zurletrectinib exhibits higher activity against most TRK inhibitor resistance mutations (13 out of 18 mutations). Zurletrectinib can be used for the study of glioma .
|
-
-
- HY-12866A
-
|
LOXO-101 sulfate; ARRY-470 sulfate
|
Trk Receptor
Apoptosis
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Cancer
|
|
Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
-
- HY-B0791
-
|
DCC-2701
|
VEGFR
c-Met/HGFR
FLT3
Trk Receptor
|
Cancer
|
|
Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.
|
-
-
- HY-15590
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AZ-23
3 Publications Verification
AZD1332
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Trk Receptor
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Cancer
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AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
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-
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- HY-137465
-
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PROTACs
Trk Receptor
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Cancer
|
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CG428 is a potent and selective CRBN-dependent tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1 phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). CG428 can be used for the research of colorectal carcinoma .
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-
-
- HY-122616
-
|
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Trk Receptor
|
Neurological Disease
|
|
PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .
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-
-
- HY-46531
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-
-
- HY-102066
-
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AZD-7451
|
Trk Receptor
|
Cancer
|
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Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors .
|
-
-
- HY-131706A
-
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Trk Receptor
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Cancer
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GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2), a TRK inhibitor, which is from the patent WO 2020038415 A1 .
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-
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- HY-107362
-
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Trk Receptor
|
Cancer
|
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CH7057288 is a potent and selective TRK inhibitor. CH7057288 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
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- HY-100695
-
|
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Discoidin Domain Receptor
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Cancer
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DDR-TRK-1, a chemical probe, is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.
|
-
-
- HY-112436
-
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Trk-IN-4
|
Trk Receptor
|
Neurological Disease
|
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PF-6683324 (Trk-IN-4) is a potent pan-Trk inhibitor in cell-based assays with
IC50s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .
|
-
-
- HY-157542
-
|
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Trk Receptor
PROTACs
|
Others
|
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CG428-NEG is a TRK degrader negative control. CG428 (HY-137465) inhibits cell growth and reduce TPM3-TRKA levels .
|
-
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- HY-112437
-
|
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Trk Receptor
|
Neurological Disease
|
|
PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with
IC50s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .
|
-
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- HY-N0020R
-
|
|
Reference Standards
Wnt
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
Echinacoside (Standard) is the analytical standard of Echinacoside. This product is intended for research and analytical applications. Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche deserticola, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity .
|
-
-
- HY-19295
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
TRK-530 sodium is an orally active bisphosphonate. TRK-530 sodium inhibits CINC-1. TRK-530 sodium inhibits dental calculus formation. TRK-530 sodium also inhibits paw edema, joint destruction and osteomyelitis .
|
-
-
- HY-144321
-
|
|
Trk Receptor
|
Cancer
|
|
Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers .
|
-
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- HY-146697
-
|
|
Trk Receptor
c-Fms
PDGFR
Bcr-Abl
c-Kit
Apoptosis
|
Cancer
|
|
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .
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-
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- HY-175271
-
|
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PROTACs
Trk Receptor
ERK
|
Cancer
|
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JWJ-01-378 is a selective TRK PROTAC degrader. JWJ-01-378 efficiently degrades WT TRK and TPM3-TRKA fusion proteins and inhibits downstream pERK signaling, while showing limited efficacy against TRK inhibitor resistant mutants and ALK fusions. JWJ-01-378 potently suppresses cancer cell proliferation .Pink: TRK ligand (HY-160520); Blue: CRBN ligase ligand (HY-103596); Black: linker
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-
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- HY-177082
-
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Trk Receptor
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Cancer
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Eratrectinib (Example 1) is a Trk inhibitor. Eratrectinib can be studied in research for tropomyosin receptor kinase-related diseases and cancers .
|
-
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- HY-124637
-
|
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Trk Receptor
|
Neurological Disease
|
|
ALE-0540, a nonpeptidic small molecule, is a nerve growth factor receptor antagonist. ALE-0540 inhibits the binding of NGF to tyrosine kinase (Trk) A or both p75 and TrkA with IC50 values of 5.88 μM and 3.72 μM, respectively. ALE-0540 can be used to examine mechanisms leading to the development of agents for the study of pain .
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-
-
- HY-174161
-
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Trk Receptor
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Cancer
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Type II TRK inhibitor 3 (Compound 18d) is a Type II TRK inhibitor with IC50 values of 0.82, 1.82, and 0.12 nM for TRKAWT/G595R/G667C, respectively. Type II TRK inhibitor 3 exhibits antitumor activity .
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-
-
- HY-120393
-
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Trk Receptor
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Cancer
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GZ-389988 is a potent pan-TRK inhibitor with IC50 values of 0.3, 0.1, and 0.5 nM for TRKA, TRKB, and TRKC, respectively. GZ-389988 can be used to study NTRK fusion-positive tumors .
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- HY-161179
-
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Trk Receptor
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Cancer
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TRK-IN-27 (Compound 14q) is a potent TRK inhibitor with good kinase selectivity. TRK-IN-27 effectively inhibits tumor growth .
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-
- HY-150258
-
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Trk Receptor
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Others
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TRK-IN-22 (compound 11) is a TRK inhibitor. TRK-IN-22 (compound 11), a typical type I inhibitor, covers the ATP-binding pocket of TRKA .
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-
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- HY-175302
-
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Trk Receptor
Apoptosis
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Cancer
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TRK-IN-32 is a potent TRK inhibitor. TRK-IN-32 potently inhibits TRK WT, TRK G595R and TRK G667C with IC50 values of 0.08 nM, 2.14 nM and 0.68 nM, respectively. TRK-IN-32 also demonstrates antiproliferative activity against a panel of Ba/F3 cell lines transformed with wild type, xDFG, solvent-front as well as gatekeeper mutant TRK fusion proteins. TRK-IN-32 induces apoptosis of Ba/F3-TRKA WT and Ba/F3-TRKA G667C cells.TRK-IN-32 can be used for the study of various cancers (such as thyroid cancer, secretory breast carcinoma) .
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- HY-160165
-
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Trk Receptor
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Cancer
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TRK-IN-25 (compound 16) is a Trk inhibitor with antiproliferative activity against cancer cells. TRK-IN-25 can be used in cancer research .
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- HY-160166
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Trk Receptor
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Cancer
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TRK-IN-26 (compound 12) is a TRK inhibitor with potential for cancer research .
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- HY-174330A
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Trk Receptor
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Cancer
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TRK-IN-31 hydrochloride is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 hydrochloride has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 hydrochloride significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
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- HY-174330
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Trk Receptor
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Cancer
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TRK-IN-31 is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
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- HY-161819
-
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Trk Receptor
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Cancer
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TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC50: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKA G595R, TRKA F589L, TRKA G667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties .
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- HY-151945
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Trk Receptor
FLT3
VEGFR
RET
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Cancer
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TRK II-IN-1 is a potent type II TRK inhibitor, with IC50s of 3.3, 6.4, 4.3 and 9.4 nM, for TRKA/B/C and TRKA G667C, respectively. TRK II-IN-1 also inhibits FLT3, RET, and VEGFR2 with IC50s of 1.3, 9.9, and 71.1 nM, respectively. TRK II-IN-1 can be used for the research of TRK driven cancers .
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- HY-144423
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Trk Receptor
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Cancer
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Trk-IN-10 (Compound 14j) is a potent inhibitor of TRK (IC50 = 0.86, 6.92 nM, against TrkA, TrkA G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key agent target in solid tumors. Trk-IN-10 (IC50 = 350 nM against ALK) has a higher selectivity of Trk inhibition, which may be of great significance for reducing toxicity .
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- HY-146115
-
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Trk Receptor
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Cancer
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TRK-IN-19 (Compound I-10 ) is a potent inhibitor of TRK (TRKA IC50 = 1.1 nM, TRKA G595R IC50 = 5.3 nM). TRK-IN-19 has the potential for the research of cancer diseases .
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- HY-146521
-
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Trk Receptor
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Cancer
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TRK-IN-15 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-15 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-55) .
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- HY-146522
-
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Trk Receptor
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Cancer
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TRK-IN-16 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-16 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-21) .
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- HY-146519
-
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Trk Receptor
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Cancer
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TRK-IN-14 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-14 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-47) .
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- HY-144424
-
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Trk Receptor
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Cancer
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Trk-IN-11 (Compound 14h) is a potent inhibitor of TRK (IC50 = 1.4, 1.8 nM, against TrkA, TrkA G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key agent target in solid tumors. Trk-IN-11 has the potential for the research of cancer disease .
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- HY-146518
-
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Trk Receptor
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Cancer
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TRK-IN-13 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-13 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-24) .
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- HY-146807
-
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Trk Receptor
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Cancer
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Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA G667C and ETV6-TRKC G696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively . Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-163004
-
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Trk Receptor
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Cancer
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Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
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-
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- HY-144732
-
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Trk Receptor
Anaplastic lymphoma kinase (ALK)
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Cancer
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TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALK WT and ALK L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases .
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- HY-12327
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-
- HY-163366
-
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Trk Receptor
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Cancer
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TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC50 values of 0.55 nM, 25.1 nM and 5.4 nM against TRK WT, TRK G595R and TRK G667C, respectively. TRK-IN-2 shows antiproliferative activity with IC50 values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKA WT, Ba/F3-ETV6-TRKB WT, Ba/F3-LMNA-TRK G595R and Ba/F3-LMNA-TRKA G667C, respectively .
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- HY-144451
-
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Trk Receptor
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Cancer
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TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line .
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- HY-168858
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Trk Receptor
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Cancer
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TRK-IN-30 (Compound C11) is the inhibitor for tropomyosin receptor kinase (TRK) that inhibits TRKA, TRKB and TRKC and drug resistant mutant TRKA G595R with an IC50 of 1.8, 0.98, 3.8, and 54 nM, respectively. TRK-IN-30 inhibits the activation of the downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 inhibits the colony formation and cell migration of Km-12, arrests the cell cycle at G0/G1 phase, and induces apoptosis in Km-12 .
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- HY-146523
-
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Trk Receptor
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Cancer
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TRK-IN-17 is a potent inhibitor of TRK. Tropomyosin-related kinases (Trks) are a family of receptor tyrosine kinases activated by neurotrophins, a group of soluble growth factors including Nerve Growth Factor (NGF), Brain-Derived Neurotrophic Factor (BDNF) and Neurotrophin-3 (NT-3) and Neurotrophin-4/5 (NT-4/5). TRK-IN-17 has the potential for the research of cancer diseases (extracted from patent WO2021148807A1, compound 3) .
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- HY-146524
-
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Trk Receptor
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Cancer
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TRK-IN-18 is a potent inhibitor of TRK. Tropomyosin-related kinases (Trks) are a family of receptor tyrosine kinases activated by neurotrophins, a group of soluble growth factors including Nerve Growth Factor (NGF), Brain-Derived Neurotrophic Factor (BDNF) and Neurotrophin-3 (NT-3) and Neurotrophin-4/5 (NT-4/5). TRK-IN-18 has the potential for the research of cancer diseases (extracted from patent WO2021148805A1, compound 7) .
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- HY-144028
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Trk Receptor
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Cancer
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Compound cpd-1 is a small molecule Trks inhibitor with good antitumor activity .
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- HY-156086
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Trk Receptor
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Cancer
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TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA G595R, TRKA G667C and TRKA F589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM .
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- HY-143561
-
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Trk Receptor
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Cancer
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Trk-IN-8 is a potent TRK inhibitor with IC50s of 0.42, 0.89 and 1.5 nM for TRKAa, TRKA(G595R) and TRKC(G623R), respectively (WO2021115401A1, compound 3) .
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- HY-144069
-
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Trk Receptor
Apoptosis
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Cancer
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Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkA G595R, TrkA G667C, TrkA G667S, TrkA F589L and TrkC G623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis .
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- HY-153745
-
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Trk Receptor
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Cancer
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Protein kinase inhibitor 5 is a potent TRK-A inhibitor with an IC50 value of 1.8 nM. Protein kinase inhibitor 5 inhibits cell viability .
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- HY-149965
-
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Trk Receptor
Apoptosis
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Cancer
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TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKA G595R, TRKA F589L, and TRKA G667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells .
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- HY-153745A
-
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Trk Receptor
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Cancer
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Protein kinase inhibitor 5 sulfate hydrate is a potent TRK-A inhibitor with an IC50 value of 1.8 nM. Protein kinase inhibitor 5 sulfate hydrate inhibits cell viability .
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- HY-143557
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Trk Receptor
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Cancer
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|
Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC50s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC50<15 nM) ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC50=5-50 nM) .
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-
- HY-153743
-
|
|
ROS Kinase
Trk Receptor
|
Cancer
|
|
Protein kinase inhibitor 4 (Compound 3) is a protein kinase inhibitor that inhibits TRK-A and ROS1 (IC50=3.0 nM and 104 nM respectively) .
|
-
- HY-147303
-
|
|
Trk Receptor
EGFR
|
Cancer
|
|
Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity .
|
-
- HY-12866B
-
|
(R)-LOXO-101; (R)-ARRY-470
|
Trk Receptor
|
Infection
Inflammation/Immunology
Cancer
|
|
(R)-Larotrectinib is a potent TRK inhibitor with an IC50 value of 28.5 nM for TrkA. (R)-Larotrectinib can be used for researching cancer, inflammatory and certain infectious diseases
|
-
- HY-132229
-
|
|
Trk Receptor
|
Cancer
|
|
LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkA G595R and TrkA G667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity .
|
-
- HY-118271
-
-
- HY-166363S
-
|
Trk-100-d3; ML 1129-d3
|
Isotope-Labeled Compounds
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Beraprost-d3 (TRK-100-d3) is deuterium labeled (Rac)-Beraprost. (Rac)-Beraprost ((Rac)-ML 1229) is an orally active prostacyclin analog that inhibits the release of Ca 2+ from intracellular storage sites by binding to prostacyclin membrane receptors (Prostaglandin Receptor), leading to relaxation of smooth muscle cells and vasodilation. Beraprost has vasodilatory, antiplatelet, and cytoprotective effects, making it promising for research in the field of cardiovascular diseases, such as thromboangiitis obliterans and atherosclerosis .
|
-
- HY-126287
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
|
-
- HY-112434
-
|
|
Trk Receptor
|
Neurological Disease
|
|
PF-06733804 is a potent pan-Trk inhibitor in cell-based assays with
IC50s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .
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-
- HY-101977R
-
|
LOXO-195 (Standard)
|
Reference Standards
Trk Receptor
|
Cancer
|
|
Selitrectinib (Standard) is the analytical standard of Selitrectinib. This product is intended for research and analytical applications. Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC50s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively .
|
-
- HY-101977B
-
|
(3aR)-LOXO-195
|
Trk Receptor
|
Cancer
|
|
(3aR)-Selitrectinib ((3aR)-LOXO-195) is an isform of Selitrectinib (HY-101977), which is a next-generation TRK kinase inhibitor, with IC50s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively .
|
-
- HY-157148
-
|
|
c-Met/HGFR
Trk Receptor
|
Cancer
|
|
1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors .
|
-
- HY-164461
-
|
|
Trk Receptor
|
Cancer
|
|
AZD6918 is an orally active and selective Trk tyrosine kinase inhibitor. AZD6918 induces cell death as a single agent and attenuates BDNF/TrkB-induced protection from Etoposide (HY-13629) in vitro. AZD6918 can be used for the research of neuroblastoma .
|
-
- HY-12866R
-
|
LOXO-101 (Standard); ARRY-470 (Standard)
|
Reference Standards
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (Standard) is the analytical standard of Larotrectinib. This product is intended for research and analytical applications. Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-112436A
-
|
|
Trk Receptor
|
Neurological Disease
Cancer
|
|
(3S,4R)-PF-6683324 is a tropomyosin-related kinase (Trk) inhibitor extracted from patent WO2015092610A1 example 9. (3S,4R)-PF-6683324 has the potential for the research of pain and cancer .
|
-
- HY-12866AR
-
|
LOXO-101 sulfate (Standard); ARRY-470 sulfate (Standard)
|
Trk Receptor
Apoptosis
Reference Standards
|
Cancer
|
|
Larotrectinib sulfate (Standard) is the analytical standard of Larotrectinib sulfate. This product is intended for research and analytical applications. Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-150561
-
|
|
Trk Receptor
|
Cancer
|
|
Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC50 values of 1.6 nM, 2.9 nM and 2.0 nM, respectively .
|
-
- HY-108263A
-
|
(S)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
|
(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML) .
|
-
- HY-10424R
-
|
PHA-848125 (Standard)
|
Reference Standards
CDK
Autophagy
|
Cancer
|
|
Milciclib (Standard) is the analytical standard of Milciclib. This product is intended for research and analytical applications. Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
|
-
- HY-146755
-
|
|
Trk Receptor
|
Cancer
|
|
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
|
-
- HY-101977A
-
|
(R,S)-LOXO-195
|
Trk Receptor
|
Cancer
|
|
(R,S)-Selitrectinib ((R,S)-LOXO-195) (compound 17) is a Trk inhibitor with activity against cancers harboring Trk inhibitor-resistant point mutations in NTRK1, NTRK2, or NTRK3 genes. (R,S)-Selitrectinib can be used for the research of trk inhibitor-resistant cancer .
|
-
- HY-180172
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
|
TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKA G667C degradation (DC50 = 24.69 nM; Dmax > 90%), while sparing the wild-type protein in virto. TRK-IN-33 shows antiproliferative activities against Ba/F3-LMNA-NTRK1 G667C cells with an IC50 value of 2.48 nM. TRK-IN-33 effectively inhibits tumor growth and enhances apoptosis in tumor tissues with no apparent toxicity in vivio. TRK-IN-33 can be used for NTRK fusion−positive cancers research .
|
-
- HY-12328
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Trk-IN-2 is an orally active pan-Trk kinase inhibitor with an TrkA IC50 of 9 nM. Trk-IN-2 exhibits pharmacodynamic effects in rat models of inflammatory pain and neuropathic pain.Trk-IN-2 can be used for the research of inflammatory pain, neuropathic pain .
|
-
- HY-181780
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-34 is an orally active TRKand TRKC mutant kinase inhibitor, with IC50 values of 0.75 nM and 0.96 nM against TRKA G595R and TRKA G667C, respectively. TRK-IN-34 inhibits the kinase activities of TRKA G595R and TRKA G667C at the functional level. TRK-IN-34 inhibits the proliferation of TRKA-transfected cells, exerts tumor growth-inhibitory effects and achieves partial tumor regression in xenograft models. TRK-IN-34 can be used to study TRK inhibitor-resistant cancers driven by the TRKA G667C mutation .
|
-
- HY-102066R
-
|
AZD-7451 (Standard)
|
Reference Standards
Trk Receptor
|
Cancer
|
|
Utatrectinib (Standard) is the analytical standard of Utatrectinib (HY-102066). This product is intended for research and analytical applications. Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors .
|
-
- HY-107362R
-
|
|
Reference Standards
Trk Receptor
|
Cancer
|
|
CH7057288 (Standard) is the analytical standard of CH7057288 (HY-107362). This product is intended for research and analytical applications. CH7057288 is a potent and selective TRK inhibitor. CH7057288 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-182335
-
|
|
Itk
Trk Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
|
PF-07245303 is a ITK/TRK inhibitor. PF-07245303 reduces the production of inflammatory cytokines such as IL-4 and IFNγ, and inhibits the phosphorylation of PLCγ1. PF-07245303 inhibits nerve growth factor-induced basophil activation and the phosphorylation of TRKA. PF-07245303 reduces oxazolone-induced ear swelling in mouse ear tissues. PF-07245303 is applicable to research related to atopic dermatitis .
|
-
- HY-103022R
-
|
TPX-0005 (Standard)
|
Reference Standards
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Repotrectinib (Standard) is the analytical standard of Repotrectinib (HY-103022). This product is intended for research and analytical applications. Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity .
|
-
- HY-181871
-
|
|
Trk Receptor
Akt
ERK
Apoptosis
|
Cancer
|
|
DZX19 (Compound C02) is an orally active, selective TRK inhibitor with a TRKA IC50 value of 1.32 nM, a TRKB IC50 of 2.28 nM, and a TRKC IC50 of 4.05 nM. DZX19 inhibits the kinase activities of wild-type TRKA, TRKA mutants (G595R, F589L, G667C), wild-type TRKB, and wild-type TRKC, and suppresses the phosphorylation of TRKA as well as its downstream AKT and ERK signaling pathways. DZX19 induces apoptosis. DZX19 inhibits tumor growth in a colorectal cancer xenograft mouse model. DZX19 is applicable for the research of colorectal cancer .
|
-
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0020
-
-
-
- HY-N6732
-
|
SF2370; Antibiotic K 252a; Antibiotic SF 2370
|
Alkaloids
Structural Classification
Microorganisms
Classification of Application Fields
Inflammation/Immunology
Disease Research Fields
Indole Alkaloids
Source Classification
|
Autophagy
PKA
PKC
Trk Receptor
CaMK
|
|
K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively . K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene .
|
-
-
- HY-N0020R
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-166363S
-
|
|
|
Beraprost-d3 (TRK-100-d3) is deuterium labeled (Rac)-Beraprost. (Rac)-Beraprost ((Rac)-ML 1229) is an orally active prostacyclin analog that inhibits the release of Ca 2+ from intracellular storage sites by binding to prostacyclin membrane receptors (Prostaglandin Receptor), leading to relaxation of smooth muscle cells and vasodilation. Beraprost has vasodilatory, antiplatelet, and cytoprotective effects, making it promising for research in the field of cardiovascular diseases, such as thromboangiitis obliterans and atherosclerosis .
|
-
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