Scientific Reviews
Product Guides
Blogs
Topics
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
11 Results for "
TRK mutant
" in MedChemExpress (MCE) Product Catalog:
Products (11)
11 Results for "TRK mutant" in MCE Product Catalog:
Cat. No.: HY-175271
Target:
Research Areas:
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
Cat. No.: HY-139891
CAS No.: 2489327-43-5
Target:
Research Areas:
Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC50 = 0.2-0.7 nM).
Cat. No.: HY-161819
Target:
Research Areas:
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-175302
CAS No.: 3044124-79-7
Target:
Research Areas:
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-144069
CAS No.: 2763637-66-5
Target:
Research Areas:
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-168858
Target:
Research Areas:
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-126287
CAS No.: 2366216-76-2
Target:
Research Areas:
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 .
Cat. No.: HY-156086
CAS No.: 2937544-01-7
Target:
Research Areas:
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-E70785
Target:
Research Areas:
TRKA is a member of the tropomyosin receptor kinase (TRK) family, and its primary binding ligand is nerve growth factor (NGF). TRKA G667C is a mutant of TRKA. TRKA G667C Recombinant Human Active Protein Kinase is a recombinant TRKA G667C protein that can be used to study TRKA G667C-related functions .
Cat. No.: HY-181780
CAS No.: 2489327-91-3
Target:
Research Areas:
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
Target:
Research Areas:
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 .
- 1
-
-
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
