150 products were found matching "K05126"!

RET is a proto-oncogene encoding a receptor tyrosine kinase. RET regulates key aspects of cellular proliferation, differentiation and survival. The activation of RET via gene fusions or point mutations is closely related to lung, thyroid and other cancers.

WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET and kinase insert domain receptor (KDR), respectively. It also inhibits EGFR (IC50 = 4 µM) and binds to tau-tubulin kinase 1 (TTBK1, Kds = 0.46 and 0.24 µM for phosphorylated and non-phosphorylated TTBK1,...

A RET inhibitor (IC50 = 0.008 µM), selective for RET over a panel of 44 serine/threonine/tyrosine kinases at 10 µM but does inhibit nine by >75%, selective for RET over a panel of 63 receptor and non-receptor tyrosine kinases 0.4 µM but does inhibit six, including RET, by >75%, reduces the proliferation of HCT116...

Protein function: Receptor tyrosine-protein kinase involved in numerous cellular mechanisms including cell proliferation, neuronal navigation, cell migration, and cell differentiation in response to glia cell line- derived growth family factors (GDNF, NRTN, ARTN, PSPN and GDF15) (PubMed:20064382, PubMed:20616503,...

A RETV804M inhibitor (IC50 = 19 nM). Formulation: A solid. InChI: InChI=1S/C18H21N5O2/c1-22(2)8-3-7-19-17-6-9-23-18(21-17)14(11-20-23)13-4-5-15-16(10-13)25-12-24-15/h4-6,9-11H,3,7-8,12H2,1-2H3,(H,19,21). InChIKey: DQYRQFLRDJTHQM-UHFFFAOYSA-N. SMILES: CN(C)CCCNC1=NC2=C(C3=CC=C4OCOC4=C3)C=NN2C=C1

LOXO-292 is an inhibitor of the receptor tyrosine kinase RET. It inhibits the phosphorylation of a KIF5B-RET fusion protein expressed in HEK293 cells (IC50 = 4 nM). LOXO-292 selectively inhibits proliferation of cancer cells containing RET mutations or gene fusions, including RETM918T-containing MZ-CRC-1 medullary...

Soluble in DMSO or ethanol. Regorafenib (BAY 73-4506, Fluoro-Sorafenib) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFR beta, Kit, RET and Raf-1 with IC(50) values of 13, 4.2, 46, 22, 7, 1.5 and 2.5nM, respectively. Target: VEGFR , Kinase Group: RTK , Substrate: Tyrosine

RPI-1 is an ATP-dependent RET kinase inhibitor. It has been shown to selectively inhibit the anchorage-independent growth of NIH3T3 cells transformed by the ret/ptc1 oncogene with an IC50 value of 0.97 µM. In a spontaneously metastasizing lung carcinoma xenograft mouse model, daily oral treatment with RPI-1 was...

Pralsetinib is an inhibitor of RET (IC50s = 0.4, 0.3, 0.4, and 0.4 nM for wild-type RET, RETV804L, RETV804M, and RETM918T, respectively). It is selective for RET over VEGFR2 (IC50 = 35 nM) and a panel of 371 kinases at 300 nM. Pralsetinib also inhibits a fusion protein of coiled-coil domain-containing protein 6 with...

Description: Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion). Target: c-RET. Smiles: CO[C@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1. References:...

Active human Ret (GenBank Accession No. NM_020975), (a.a. 658-end) with N-terminal GST tag, MW= 77.5 kDa, expressed in an Baculovirus infected Sf9 cell expression system.