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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
45 Results for "
Trk kinase inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (45)
45 Results for "Trk kinase inhibitors" in MCE Product Catalog:
27
27 Publications Verification
Cat. No.: HY-N6732
CAS No.: 99533-80-9
Synonyms: SF2370; Antibiotic K 252a; Antibiotic SF 2370
Target:
17
17 Cited Publications
Synonyms: LOXO-101; ARRY-470
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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).
17
17 Cited Publications
Synonyms: LOXO-101 sulfate; ARRY-470 sulfate
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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).
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.
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
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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) .
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.
1
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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.
Cat. No.: HY-148811
CAS No.: 2403703-30-8
Synonyms: ICP-723
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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 .
Cat. No.: HY-137465
CAS No.: 2412055-93-5
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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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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 .
Cat. No.: HY-46531
CAS No.: 2412056-27-8
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Thalidomide-5-NH2-CH2-COOH (compound 114) is a potent and selective inhibitor of tropomyosin receptor kinase (trk). Thalidomide-5-NH2-CH2-COOH is a ligand of E3 ligase. Thalidomide-5-NH2-CH2-COOH has the potential for researching one or more diseases (extracted from patent WO2021170109A1) .
Cat. No.: HY-146697
CAS No.: 2416844-79-4
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 .
Cat. No.: HY-177082
CAS No.: 2396516-98-4
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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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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 .
Cat. No.: HY-161179
CAS No.: 3032924-03-8
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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 .
Cat. No.: HY-144424
CAS No.: 2700265-62-7
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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 .
Cat. No.: HY-144423
CAS No.: 2700265-61-6
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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 .
Cat. No.: HY-12327
CAS No.: 1402438-37-2
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Trk-IN-1 (example 9), a potent tropomyosin-related kinase (Trk) inhibitor, shows potency against TrkA (3.7 nM) and TrkB (94 nM), respectively .
Cat. No.: HY-153745
CAS No.: 2278204-94-5
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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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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
