Search Result

Results for "

G667C

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (6) E3 Ligase Ligand-Linker Conjugates (1) ERK (1) FLT3 (1) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (1) PROTACs (1) RET (1) Trk Receptor (21) VEGFR (1)
By Research Areas:	Cancer (21)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-E70785

*TRKA G667C* Recombinant Human Active Protein Kinase**	Trk Receptor	Cancer
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 .

HY-174330A

TRK-IN-31 hydrochloride	Trk Receptor	Cancer
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 .

HY-174330

TRK-IN-31	Trk Receptor	Cancer
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 .

HY-132229

LPM4870108	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-156086

TRK-IN-24	Trk Receptor	Cancer
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 .

HY-175302

TRK-IN-32	Trk Receptor Apoptosis	Cancer
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) .

HY-163366

TRK-IN-28	Trk Receptor	Cancer
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 .

HY-174161

Type II TRK inhibitor 3	Trk Receptor	Cancer
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 .

HY-126287

JND4135	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-144069

Pan-Trk-IN-3	Trk Receptor Apoptosis	Cancer
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 .

HY-161819

TRK-IN-29	Trk Receptor	Cancer
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 .

HY-149965

TRK-IN-23	Trk Receptor Apoptosis	Cancer
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 .

HY-151945

TRK II-IN-1	Trk Receptor FLT3 VEGFR RET	Cancer
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 .

HY-163004

Type II TRK inhibitor 2	Trk Receptor	Cancer
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 .

HY-146755

TIY-7	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-181780

TRK-IN-34	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-181052

PROTAC NTRK1 degrader-1	PROTACs Trk Receptor	Cancer
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 .

HY-146807

Type II TRK inhibitor 1	Trk Receptor	Cancer
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.

HY-180172

TRK-IN-33	Trk Receptor Apoptosis	Cancer
TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKA ^G667C degradation (DC₅₀ = 24.69 nM; D_max > 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-181871

DZX19	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 .

HY-W1115186

CRBN ligand-900	Ligands for E3 Ligase	Others
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) .

HY-185546

CRBN ligand-900 Gly	E3 Ligase Ligand-Linker Conjugates	Others
CRBN ligand-900 Gly is a synthesized E3 ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugate) that incorporates a CRBN ligand and a linker. CRBN ligand-900 Gly can be connected to the target protein ligand to form a PROTAC NTRK1 degrader-1 (HY-181052) .

HY-185545

NTRK1-ligand-1	Ligands for Target Protein for PROTAC Trk Receptor	Cancer
NTRK1-ligand-1 (Compound 15) is a NTRK1 ligand. NTRK1-ligand-1 serves as a Ligand for Target Protein for PROTAC, which is applicable to the development and design of PROTAC NTRK1 degraders, such as PROTAC NTRK1 degrader-1 (HY-181052). NTRK1-ligand-1 can be used in the research of solid tumors .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Name
Email *

	Sorry, but the email address you supplied was invalid.

G667C

Inhibitors & Agonists