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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
85 Results for "
TrkA kinase
" in MedChemExpress (MCE) Product Catalog:
Products (85)
85 Results for "TrkA kinase" in MCE Product Catalog:
17
17 Publications Verification
Synonyms: LOXO-101; ARRY-470
Target:
Research Areas:
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).
17
17 Publications Verification
Synonyms: LOXO-101 sulfate; ARRY-470 sulfate
Target:
Research Areas:
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).
13
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BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases .
12
12 Cited Publications
Cat. No.: HY-18314
CAS No.: 504433-23-2
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GW 441756 is a potent and specific nerve growth factor (NGF) receptor tyrosine kinases A (TrkA) inhibitor (IC50=2 nM), which eliminates the BmK NSPK-induced neurite outgrowth .
7
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.
6
Research Areas:
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with 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 . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
5
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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 .
4
4 Cited Publications
Target:
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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) .
4
Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .
3
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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.
3
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Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity .
1
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Belizatinib (TSR-011) is an orally active, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
1
1 Cited Publications
Cat. No.: HY-P76116
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: NTRK1; Tyrosine kinase Receptor A; Neurotrophic Receptor Tyrosine kinase 1; P140-TrkA; TrkA; Gp140trk; TRK; Trk-A; MTC; Neurotrophic Tyrosine kinase Receptor Type 1; High Affinity Nerve Growth Factor Receptor; Tyrosine-Protein kinase Receptor; Neurotrophi
Species:
Mouse
Source:
HEK293
1
1 Cited Publications
Cat. No.: HY-P7308
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: NTRK1; Tyrosine kinase Receptor A; Neurotrophic Receptor Tyrosine kinase 1; P140-TrkA; TrkA; Gp140trk; TRK; Trk-A; MTC; Neurotrophic Tyrosine kinase Receptor Type 1; High Affinity Nerve Growth Factor Receptor; Tyrosine-Protein kinase Receptor; Neurotrophic Tyrosine kinase, Receptor, Type 1; Tyrosine kinase Receptor; TRK1-Transforming Tyrosine kinase Protein; Oncogene TRK; Tropomyosin Receptor kinase A; TRK1; Tropomyosin-Related kinase A
Species:
Human
Source:
HEK293
Cat. No.: HY-P99297
CAS No.: 2171034-69-6
Synonyms: ZTS-00508841
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Cat. No.: HY-148811
CAS No.: 2403703-30-8
Synonyms: ICP-723
Target:
Research Areas:
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 .
Cat. No.: HY-137465
CAS No.: 2412055-93-5
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Research Areas:
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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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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Research Areas:
DLK-IN-1 (Compound 14) is an orally active, blood-brain barrier-penetrable and selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a Ki value of 3 nM. DLK-IN-1 inhibits Flt3, PAK4, STK33 and TrkA. DLK-IN-1 reduces p-c-Jun. DLK-IN-1 can be used in Alzheimer's disease research .
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TrkA-IN-1 is a potent and selective Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 of 99 nM in a cell-based assay. TrkA-IN-1 has analgesic activity .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
