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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
22 Results for "
G595R
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "G595R" in MCE Product Catalog:
Cat. No.: HY-132229
CAS No.: 2803679-07-2
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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 .
Cat. No.: HY-144451
CAS No.: 2823342-34-1
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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 .
Cat. No.: HY-146115
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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 .
Cat. No.: HY-143561
CAS No.: 2762200-57-5
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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) .
Cat. No.: HY-156086
CAS No.: 2937544-01-7
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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 .
Cat. No.: HY-163366
CAS No.: 2991504-43-7
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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 .
Cat. No.: HY-174161
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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 .
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-144069
CAS No.: 2763637-66-5
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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 .
Cat. No.: HY-149965
CAS No.: 2924344-29-4
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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 .
Cat. No.: HY-161819
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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 .
Cat. No.: HY-146755
CAS No.: 2846435-83-2
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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 .
Cat. No.: HY-163004
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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 .
Cat. No.: HY-181052
CAS No.: 2922274-35-7
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PROTAC NTRK1 degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). PROTAC NTRK1 degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1. PROTAC NTRK1 degrader-1 can be used for the research of solid tumors .
Cat. No.: HY-168858
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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 .
Cat. No.: HY-175302
CAS No.: 3044124-79-7
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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) .
Cat. No.: HY-181780
CAS No.: 2489327-91-3
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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 .
Cat. No.: HY-181871
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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.: HY-W1115186
CAS No.: 2259851-44-8
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CRBN ligand-900 is an E3 ligase ligand that can be used in the recruitment of CRBN protein. CRBN ligand-900 can be connected to the NTRK1 ligand (HY-185545) by a linker to synthesis of PROTAC NTRK1 degrader-1 (HY-181052) .
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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
