c-RET

RET-IN-23 is an orally available and highly potent RET inhibitor with significant antitumor activity for the study of non-small cell lung cancer.

RET-IN-3 is a RETV804M kinase inhibitor with potential anticancer activity for the study of non-small cell lung cancer.

TG-89 is an inhibitor of JAK2, JAK3, RET and FLT3, and has an IC50 value of 11.2 μM against JAK2, showing anticancer activity in the treatment of ovarian and

Pz-1 is an inhibitor of VEGFR2 and RET (rearranged during transfection) tyrosine kinase that blocks the blood supply required for RET-stimulated growth.

RET-IN-24 (Compound 26) is a selective inhibitor of RET tyrosine kinase, demonstrating antitumor activity [1].

NSC194598 is a p53 DNA-binding inhibitor, demonstrating an in vitro IC50 of 180 nM and an in vivo range of 2-40 μM.

RET-IN-13: potent quinoline RET inhibitor; IC50 = 0.5 nM (WT), 0.9 nM (V804M); potential for RET-related tumor/intestinal disease research.

FHND5071, a potent and selective RET kinase inhibitor, exerts antitumor effects through the inhibition of RET autophosphorylation and may be utilized for tumor

RET-IN-5 is a potent inhibitor of RET (IC50: 4.57 nM).

RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor that demonstrates efficacy against medullary thyroid carcinoma (MTC), exhibiting half-maximal

FLT3/ITD-IN-4 inhibits FLT3-ITD mutations in acute myeloid leukemia (IC50: 2.3 nM).

RET-IN-17 inhibits RET kinase; may help in IBS pain and RET-activated cancers.

RET-IN-10: Potent RET inhibitor, may treat congenital megacolon and tumors (Patent WO2021135938A1, compound 18).

WF-47-JS03: RET kinase inhibitor, crosses blood-brain barrier, 500x more selective for KDR, IC50: 1.7 nM in Ba/F3 cells, 5.3 nM in LC-2/ad lung cancer cells.

RET-IN-7 exhibits strong inhibitory effects against RET kinase in vitro and shows significant efficacy in treating RET-driven tumor xenografts in mice through

CDD-2212 is an STK33 inhibitor with a Kd of 1.9 nM and an IC50 of 999 nM. It exhibits weak inhibitory activity against off-target kinases, with IC50 values of 3223 nM for CLK1, 1555 nM for CLK2, 5884 nM for CLK4, and 1093 nM for RET. CDD-2212 is applicable in contraceptive research.

TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM).

RET-IN-30 (Compound 28) is a RET inhibitor that exhibits inhibitory activity against both wild-type RET and some of its mutants. It is capable of inhibiting the proliferation of A549 cells and demonstrates antitumor properties.

FHND5071 (1H) is a selective inhibitor of RET (rearranged during transfection) tyrosine kinase. It shows potential for research applications in RET-driven cancers, such as thyroid and lung cancer.

APS03118 is an orally effective, potent, and highly selective RET inhibitor. It broadly inhibits RET fusions and various mutations (including G810, V804, L730, and Y806 variants), with IC50 values generally below 1 nM (0.0952 nM for the wild type; mutation IC50s range from 0.00438 to 5.72 nM), demonstrating significant inhibitory activity against RETG810 mutations. APS03118 effectively suppresses the entire RET signaling pathway, including RET, Shc, and ERK1/2, and shows more than 20-fold selectivity over most off-target kinases, excluding FLT3 and YES. In vivo, APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804M PDX mouse models and significantly extends survival in intracranial CCDC6-RET metastatic mouse models. This compound is applicable for research on RET-driven cancers resistant to selective RET inhibitors (SRI).