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Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4 5.2 nM). Lenvatinib has strong anti-tumor activity.

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035 1.3 4.6 7 11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

JNJ-38158471 (CS-2660), a highly selective, orally available, well tolerated VEGFR2 inhibitor with IC50 of 40 nM, inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM.

Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A Aurora B Aurora C (IC50s: 120 nM 7 nM 1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).

WHI-P180 (Janex 3) is a potent inhibitor of EGFR and Cdk2, with IC50 values of 4.0 µM and 1.0 µM, respectively.

TG101209 is a selective JAK2 inhibitor with an IC50 of 6 nM.

Treprostinil Sodium (UT-15) is a potent DP1, IP and EP2 agonist (EC50: 0.6 1.9 6.2 nM).

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.

PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.

ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR VEGFR2, Flt4 VEGFR3, FGFR1, FGFR2, Src, PDGFRα.

Compound TPX-0046 is an inhibitor of RET. Compound TPX-0046 can inhibit the RET autophosphorylation. Compound TPX-0046 can be used for the research of cancer.

Enbezotinib is an inhibitor of RET autophosphorylation and can be used in cancer research.

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-5 is a potent inhibitor of RET with an IC50 of 4.57 nM.

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

RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor effective against medullary thyroid carcinoma (MTC), with half-maximal inhibitory concentrations (IC50s) of 3.6 μM at 3 days and 3.0 μM at 6 days in TT(C634R) MTC [1].

RET-IN-20, a potent RET inhibitor, demonstrates an IC50 value of 13.7 nM and effectively decreases the expression of p-Ret and p-Shc protein. Moreover, it induces apoptosis and exhibits antiproliferative and anti-tumor activity.

RET-IN-22 (compound 17b) is a potent, selective, and orally active inhibitor of RET, exhibiting IC50 values of 20.9 nM for wild-type RET and 18.3 nM for RET-V804M. It demonstrates a highly selective inhibition profile across a broad spectrum of kinases, with notable specificity over EGFR and VEGFR2, and is implicated in exerting anticancer effects [1].

RET-IN-15 is an inhibitor of rearrangement kinase (RET) during transfection and can be used in cancer research.