c-Ret

Cat. No.

A34872

CAS No.

2216753-97-6

Zeteletinib

Synonyms: BOS-172738; DS-5010

Zeteletinib is a selective RET kinase inhibitor that demonstrates exceptional potency against wild type RET and RETV804M/L gatekeeper mutants, as well as the frequently encountered oncogenic mutation M918T. This orally active compound exhibits nanomolar affinity for RET while maintaining over 300-fold selectivity for VEGFR2. Zeteletinib is recognized for its robust antitumor activity, making it a valuable tool in cancer research and therapeutic development focused on RET-driven malignancies.

Cat. No.

A34882

CAS No.

2375837-06-0

Zeteletinib hemiadipate

Synonyms: BOS-172738 hemiadipate; DS-5010 hemiadipate

Zeteletinib hemiadipate is a selective RET kinase inhibitor that acts with nanomolar potency against the RET protein, displaying over 300-fold selectivity for RET over VEGFR2. This compound is effective against wild type RET, as well as RETV804M/L gatekeeper mutants and the prevalent oncogenic mutation M918T. Zeteletinib hemiadipate demonstrates significant antitumor activity, making it a valuable tool for researching RET-related malignancies and potential therapeutic interventions.

Cat. No.

A34913

CAS No.

1093380-42-7

AD57

AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases.

Cat. No.

A34948

CAS No.

2320261-72-9

AD57 hydrochloride

AD57 hydrochloride is a multikinase inhibitor that targets RET, BRAF, S6K, and Src pathways. This orally active compound demonstrates significant biological activity in modulating aberrant signaling pathways associated with various cancers. Research applications include studying the effects of combined inhibition on tumor growth and resistance mechanisms in cancer cell lines and animal models.

Cat. No.

A35107

CAS No.

2598870-24-5

APS03118

APS03118 is a potent and selective inhibitor of the rearranged during transfection (RET) oncogene, targeting various RET fusions and mutations, including G810, V804, L730, and Y806, with IC50 values primarily below 1 nM. This compound effectively inhibits the entire RET signaling cascade, including RET itself, Shc, and ERK1/2, while displaying over 20-fold selectivity against most off-target kinases. In preclinical studies, APS03118 demonstrated the ability to induce complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient-derived xenografts and significantly extend survival in models of intracranial CCDC6-RET metastasis. This reagent is suitable for research into RET-driven cancers, particularly in the context of selective RET inhibitor-resistant scenarios.

Cat. No.

A35112

CAS No.

2414909-94-5

RET V804M-IN-1

RET V804M-IN-1 is a selective inhibitor targeting the RETV804M kinase, with an IC50 of 20 nM. This compound demonstrates potent inhibition of wild-type RET, making it a valuable tool for studying RET-mediated signaling pathways. Its specificity for RETV804M positions it as an important reagent for research applications in cancer biology and targeted therapies.

Cat. No.

A35114

CAS No.

2359649-81-1

Enbezotinib

Synonyms: TPX-0046

Enbezotinib is a potent RET inhibitor that effectively hinders RET autophosphorylation. This compound demonstrates significant biological activity against various cancers driven by RET alterations. It is suitable for research applications focused on cancer biology and therapeutic targeting of RET-driven malignancies.

Cat. No.

A35116

CAS No.

2561413-77-0

WF-47-JS03

WF-47-JS03 is a highly selective RET kinase inhibitor, exhibiting IC50 values of 1.7 nM and 5.3 nM in KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. It demonstrates exceptional brain penetrance and over 500-fold selectivity against kinase insert domain receptor (KDR). This compound is valuable for research applications focused on RET-driven oncogenesis and potential therapeutic strategies for RET-positive malignancies.

Cat. No.

A35117

CAS No.

2380-63-4

Pyrazoloadenine

Pyrazoloadenine is a selective inhibitor of the RET (REarranged during Transfection) oncoprotein, involved in various cancer signaling pathways. It demonstrates significant anticancer activity, particularly in lung cancer models. This compound is useful in research focused on targeted therapies for RET-driven malignancies, enabling the exploration of its effects on tumor growth and resistance mechanisms.

Cat. No.

A35118

CAS No.

2414374-53-9

RET-IN-3

RET-IN-3 is a selective RETV804M kinase inhibitor, displaying an IC50 value of 19 nM. This compound exhibits potent inhibition of RET signaling pathways, making it a valuable tool for investigating RET-driven oncogenesis. RET-IN-3 is suitable for research applications focused on cancer biology, particularly in studies targeting RET mutations.

Cat. No.

A35120

CAS No.

2436473-55-9

RET-IN-4

RET-IN-4 is a potent and selective RET inhibitor that demonstrates oral bioavailability, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM against wild-type RET, RET V804M, and RET M918T variants, respectively. This compound exhibits improved selectivity against kinases such as JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 is primarily utilized in cancer research, highlighting its potential for therapeutic applications in RET-driven malignancies.

Cat. No.

A35121

CAS No.

2643375-86-2

RET-IN-15

RET-IN-15 is a potent inhibitor of the rearranged during transfection (RET) kinase. It demonstrably impedes RET signaling pathways, contributing to the inhibition of tumor cell proliferation in various cancers. This compound is suitable for research applications exploring the role of RET in oncogenesis and therapeutic interventions targeting RET-driven malignancies.

Cat. No.

A35123

CAS No.

2715208-83-4

RET-IN-6

RET-IN-6 is a potent inhibitor of RET (rearranged during transfection) with an IC50 value of 4.57 nM. This compound effectively blocks RET signaling pathways, making it a valuable tool for research on RET-driven cancers and other related diseases. Its high specificity and efficacy facilitate investigations into therapeutic options for malignancies characterized by RET alterations.

Cat. No.

A35124

CAS No.

2546116-88-3

Soxataltinib

Soxataltinib is a potent RET-kinase inhibitor, exhibiting an IC50 of 0.601 nM. This compound is instrumental in cancer research, particularly in the study of RET-driven malignancies. Its ability to selectively inhibit RET-kinase makes it a valuable tool for investigating therapeutic strategies targeting RET-related pathways.

Cat. No.

A35126

CAS No.

2259657-48-0

RET-IN-16

RET-IN-16 is a potent and selective inhibitor of the RET receptor tyrosine kinase, exhibiting IC50 values of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM, and 8.86 nM against RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6, and RET-KIF5B, respectively. This compound demonstrates significant anticancer activity, making it a valuable tool for research in RET-related malignancies and therapeutic applications. Its selectivity and potency facilitate studies on RET-driven signaling pathways and potential treatment strategies in oncology.

Cat. No.

A35127

CAS No.

2583767-68-2

RET-IN-24

RET-IN-24 is a selective inhibitor of the RET tyrosine kinase, demonstrating significant antitumor activity. This compound is valuable in research focused on targeting RET-related signaling pathways in cancer, contributing to the understanding of tumorigenesis and potential therapeutic strategies. Its specificity allows for detailed investigations into RET-dependent malignancies.

Cat. No.

A35128

CAS No.

2479961-46-9

RET-IN-23

RET-IN-23 is a potent and orally active inhibitor of the RET protein, exhibiting IC50 values of 1.32 nM for RET-WT, 2.50 nM for RET-CCDC6, 6.54 nM for RET-V804L, 1.03 nM for RET-V804M, and 1.47 nM for RET-M918T. This compound demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic applications targeting RET-driven malignancies. Its selective inhibition profile positions RET-IN-23 as a promising candidate for further development in oncology studies.

Cat. No.

A35129

CAS No.

2965703-02-8

RET-IN-25

RET-IN-25 is a potent RET kinase inhibitor demonstrating significant anticancer activity. It effectively inhibits medullary thyroid carcinoma (MTC) cell lines, exhibiting IC50 values of 3.6 μM and 3.0 μM after 3 and 6 days of treatment, respectively, against the TT(C634R) MTC model. This compound is relevant for research in cancer therapeutics, particularly in studies targeting RET-mediated pathways in MTC.

Cat. No.

A35130

CAS No.

2649418-11-9

RET-IN-9

RET-IN-9 is a potent inhibitor of RET (rearranged during transfection) kinase, a receptor tyrosine kinase crucial for the development of the kidney and enteric nervous system. This compound demonstrates significant biological activity by targeting RET, making it a valuable tool in the study of RET-related disorders, including non-small cell lung cancer and medullary thyroid cancer. Its application in research can deepen the understanding of RET's role in various physiological systems and disease states.

Cat. No.

A35131

CAS No.

2491726-04-4

RET-IN-31

RET-IN-31 is a selective inhibitor of RET, demonstrating high potency with IC50 values of 1.4 nM for RETWT, 1.9 nM for RETV804L, and 3.8 nM for RETV804M. This compound exhibits anti-cancer activity against malignancies driven by activated RET mutations and gene fusions. Additionally, RET-IN-31 has been characterized for its inhibitory effects on hERG and various Cytochrome P450 enzymes, making it a valuable tool for exploring RET-related signaling pathways in cancer research.

Cat. No.

A35133

CAS No.

2684258-54-4

RET-IN-13

RET-IN-13 is a potent inhibitor of the RET proto-oncogene, exhibiting IC50 values of 0.5 nM for wild-type RET and 0.9 nM for the RET V804M mutant. This quinoline compound demonstrates significant efficacy in targeting RET-mediated signaling pathways, making it a valuable tool for investigating tumors and intestinal diseases associated with aberrant RET activation. Its application in research may provide insights into the therapeutic potential of RET inhibition in various oncological and gastrointestinal conditions.

Cat. No.

A35134

CAS No.

2763386-05-4

RET-IN-7

RET-IN-7 is a selective inhibitor of the RET kinase signaling pathway. It exhibits significant inhibition of RET activity in vitro and shows strong efficacy in vivo in models of RET-driven tumors following prolonged dosing in murine xenograft studies. This compound is valuable for research into targeted therapies for cancers associated with RET mutations and alterations.

Cat. No.

A35135

CAS No.

2479961-45-8

RET-IN-28

RET-IN-28 is a selective inhibitor of the RET (rearranged during transfection) receptor tyrosine kinase. It effectively targets and inhibits the activity of the mutant RET enzyme, specifically RET-V804M, making it valuable for investigations into oncogenic signaling pathways. This compound is primarily utilized in cancer research to study the role of RET mutations in tumorigenesis and therapeutic resistance.

Cat. No.

A35136

CAS No.

1885880-08-9

RET-IN-17

RET-IN-17 is a highly selective inhibitor of the RET receptor tyrosine kinase. It exhibits significant potential for investigating pain mechanisms associated with irritable bowel syndrome (IBS) and other gastrointestinal disorders, as well as for researching cancers characterized by aberrant RET kinase activity. This compound provides a valuable tool for further elucidating the biological functions and therapeutic implications of RET signaling pathways.

Cat. No.

A35137

CAS No.

2918281-79-3

RET-IN-22

RET-IN-22 is a potent and selective inhibitor of the RET kinase, exhibiting an IC50 of 20.9 nM for wild-type RET and 18.3 nM for the RET-V804M mutant. This compound demonstrates a high degree of selectivity against a range of kinases, particularly EGFR and VEGFR2. RET-IN-22 is utilized in cancer research due to its significant anticancer activity, making it a valuable tool for investigating RET-driven malignancies.