TrkA Inhibitor

TrkA Inhibitors (63):

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-145587

Paltimatrectinib	Inhibitor	99.95%
Paltimatrectinib (compound I-147) is a potent tyrosine kinase inhibitor with an IC₅₀ of <10 nM for tropomyosin kinases A (TrkA). Paltimatrectinib has the potential for cancer and inflammatory diseases.

HY-151949

TrkA-IN-4	Inhibitor	98.99%
TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a proagent of TrkA-IN-3 (IC₅₀=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects.

HY-112437

PF-06737007	Inhibitor	99.90%
PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.

HY-114357A

DS-1205b free base	Inhibitor	99.92%
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC₅₀ of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC₅₀s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.

HY-129634

TrkA-IN-1	Inhibitor
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.

HY-112423

CE-245677	Inhibitor	98.00%
CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC₅₀s of 4.7 and 1 nM.

HY-P991622

MNAC13	Inhibitor
MNAC13 is a kind of mouse IgG1 chimeric antibody, targeting to human TrkA. MNAC13 inhibits the NGF dependent signaling pathway by specifically binding to TrkA receptors. MNAC13 has good analgesic effect and long-lasting efficacy. MNAC13 can be used for researches on inflammatory and chronic pain.

HY-149912

CZS-241	Inhibitor
CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC₅₀=2.6 nM). CZS-241 inhibits TRKA with an IC₅₀ value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines.

HY-16961A

Sitravatinib malate	Inhibitor
Sitravatinib malate (MGCD516 malate) 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 malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

HY-132229

LPM4870108	Inhibitor
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-146749

FLT3/TrKA-IN-1	Inhibitor
FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC₅₀s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML).

HY-112434

PF-06733804	Inhibitor
PF-06733804 is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.

HY-123237

KRC-108	Inhibitor
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC₅₀s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice.

HY-181871

DZX19	Inhibitor
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-143557

Trk-IN-7	Inhibitor
Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC₅₀s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC₅₀<15 nM) ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC₅₀=5-50 nM).

HY-144732

TRK/ALK-IN-1	Inhibitor
TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC₅₀ values of 2.2, 9.3 and 38 nM towards TRKA, ALK^WT and ALK^L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases.

HY-143561

Trk-IN-8	Inhibitor
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).

HY-150561

Trk-IN-20	Inhibitor
Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC₅₀ values of 1.6 nM, 2.9 nM and 2.0 nM, respectively.

HY-149965

TRK-IN-23	Inhibitor
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-120393

GZ-389988	Inhibitor	99.10%
GZ-389988 is a potent pan-TRK inhibitor with IC₅₀ values of 0.3, 0.1, and 0.5 nM for TRKA, TRKB, and TRKC, respectively. GZ-389988 can be used to study NTRK fusion-positive tumors.

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