c-Ret

Cat. No.

A10250

CAS No.

755037-03-7

Regorafenib (BAY 73-4506)

Synonyms: BAY 73-4506

Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.

Cat. No.

A10715

CAS No.

827318-97-8

Danusertib (PHA-739358)

Synonyms: PHA-739358

Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2

Cat. No.

A11180

CAS No.

936091-14-4

TG101209

TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells.

Cat. No.

A11546

CAS No.

835621-07-3

Regorafenib Hydrochloride

Synonyms: BAY73-4506 hydrochloride

Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

Cat. No.

A13832

CAS No.

269730-03-2

RPI-1

RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor.

Cat. No.

A15218

CAS No.

1019206-88-2

Regorafenib monohydrate

Synonyms: BAY 73-4506 monohydrate

Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

Cat. No.

A17567

CAS No.

857890-39-2

Lenvatinib mesylate

Synonyms: E7080 mesylate; E 7080

Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

Cat. No.

A18637

CAS No.

2152628-33-4

Selpercatinib (LOXO-292)

Synonyms: LOXO292

Selpercatinib is a tyrosine kinase inhibitor with antineoplastic properties.

Cat. No.

A19015

CAS No.

2222755-14-6

RET-IN-1

RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .

Cat. No.

A19332

CAS No.

1384071-99-1

AD80

AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

Cat. No.

A19526

CAS No.

2097132-94-8

Pralsetinib

Synonyms: BLU-667

Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor.

Cat. No.

A19812

CAS No.

1357349-91-7

SPP-86

SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM.

Cat. No.

A20434

CAS No.

1627856-64-7

GSK3179106

GSK3179106 is a potent and selective RET kinase inhibitor with an IC50 of 0.4 nM.

Cat. No.

A21039

CAS No.

882405-89-2

BBT594

Synonyms: NVP-BBT594

BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.

Cat. No.

A21503

CAS No.

1055986-67-8

Amuvatinib hydrochloride

Synonyms: MP470 hydrochloride; MP 470; HPK 56 hydrochloride; HPK56

Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret.

Cat. No.

A21586

CAS No.

2097132-93-7

cis-Pralsetinib

Synonyms: cis-BLU-667; BLU667

cis-Pralsetinib (cis-BLU-667) is a highly potent and selective inhibitor of rearranged during transfection (RET), with IC50s ranging from 0.3 to 0.4 nM for WT RET and four enzyme variants (V804L, V804M, M918T, CCDC6-RET), and with broad, robust and anti-tumor activity against multiple RET-driven solid tumor types.

Cat. No.

A28577

CAS No.

153437-55-9

WHI-P180 hydrochloride

Synonyms: Janex 3 hydrochloride

WHI-P180 hydrochloride is a potent RET inhibitor that also targets KDR and EGFR. With IC50 values of 5 nM for RET, 66 nM for KDR, and 4 μM for EGFR, it demonstrates significant inhibitory activity across these kinases. This compound is widely utilized in research focused on cancer biology, particularly in studies investigating RET-driven tumors and endothelial growth signaling pathways.

Cat. No.

A28697

CAS No.

2484919-71-1

RET-IN-19

RET-IN-19 is a potent inhibitor of the RET receptor tyrosine kinase, exhibiting IC50 values of 6.8 nM for RET wild-type and 13.51 nM for the RET V804M mutant. This compound demonstrates significant anticancer activity, making it a valuable tool in the study of non-small cell lung cancer (NSCLC). RET-IN-19 is suitable for research focused on targeted therapy and the mechanisms of RET-mediated oncogenesis.

Cat. No.

A30404

CAS No.

2129515-96-2

Vepafestinib

Synonyms: TAS0953/HM06

Vepafestinib is a selective, orally active RET inhibitor that demonstrates a potent inhibitory effect with an IC50 value of 0.33 nM. By inhibiting the phosphorylation of RET and its downstream signaling pathways, Vepafestinib effectively blocks tumor cell proliferation and induces cell cycle arrest and apoptosis. This compound is valuable for research on RET-driven malignancies, including non-small cell lung cancer and thyroid cancer, among other applications in oncology.

Cat. No.

A32530

CAS No.

2764891-88-3

RET-IN-11

RET-IN-11 is a potent and selective inhibitor of the RET receptor tyrosine kinase, exhibiting IC50 values of 6.20 nM for RET and 18.68 nM for the RETV804M mutation. This compound demonstrates significant anti-proliferative and anti-migratory effects in CCDC6-RET-driven LC-2/ad cells. Additionally, RET-IN-11 promotes apoptosis, making it a valuable tool for research in cancer biology and targeted therapies for RET-related malignancies.

Cat. No.

A34470

CAS No.

2755843-62-8

RET-IN-14

RET-IN-14 is a highly selective RET inhibitor that demonstrates potent inhibition with IC50 values of less than 0.51 nM for wild-type RET and varying nanomolar activity against RET mutations (G810R and V804M) as well as BTK and its C481S mutant. Its exceptional efficacy positions RET-IN-14 as a valuable tool for investigating RET-driven tumors and exploring therapeutic strategies in cancer research.

Cat. No.

A34578

CAS No.

1613437-66-3

KBP-7018

KBP-7018 is a selective tyrosine kinase inhibitor targeting c-KIT, PDGFR, and RET. It demonstrates potent inhibition with IC50 values of 10 nM for c-KIT, 7.6 nM for PDGFR, and 25 nM for RET. This compound is valuable for investigating the molecular mechanisms and potential treatments related to idiopathic pulmonary fibrosis.

Cat. No.

A34584

CAS No.

1613437-67-4

KBP-7018 hydrochloride

KBP-7018 hydrochloride is a selective inhibitor of tyrosine kinases, specifically targeting c-KIT, PDGFR, and RET. It exhibits significant inhibitory potency, with IC50 values of 10 nM, 7.6 nM, and 25 nM, respectively. This compound is utilized in research focused on idiopathic pulmonary fibrosis, facilitating investigations into pathways associated with this condition.

Cat. No.

A34749

CAS No.

1800505-64-9

Pz-1

Pz-1 is a highly selective inhibitor of the RET kinase, exhibiting an IC50 of less than 1 nM against the wild type enzyme. It also effectively inhibits VEGFR2, making it a valuable reagent for studying the role of RET in oncogenic signaling pathways. Pz-1 is particularly relevant for research applications involving cancer therapy and angiogenesis.

Cat. No.

A34863

CAS No.

2760195-67-1

SYHA1815

SYHA1815 is a potent, orally bioavailable RET inhibitor, exhibiting an IC50 of 0.9 nmol/L. This compound demonstrates high selectivity for RET over KDR, with an IC50 of 15.9 nmol/L. SYHA1815 effectively arrests the G1 phase of the cell cycle and inhibits RET-driven cell proliferation by downregulating c-Myc, making it a valuable tool in cancer research and potential therapeutic applications targeting RET-related malignancies.