RET Inhibitor

RET-IN-5 is a potent RET (rearranged during transfection) inhibitor with an IC₅₀s of 0.4 nM and 135.1 nM for RET and VEGFR2, respectively (WO2021213476A1, compound 18).

RET-IN-18 is a pyridone compound. is a potent inhibitor of RET. RET-IN-18 is a potent inhibitor of RET. RET-IN-18 has the potential for the research of diseases related to irritable bowel syndrome (IBS) and other gastrointestinal disorders, as well as cancers, and neurodegenerative diseases (extracted from patent WO2022017524A1, compound 1).

CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC₅₀ values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC₅₀ values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research.

Regorafenib-¹³C,d₃ is the ¹³C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.

Selpercatinib (Standard) is the analytical standard of Selpercatinib. This product is intended for research and analytical applications. Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC₅₀ values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity.

WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC₅₀s of 5 nM, 66 nM and 4 μM, respectively.

HG-6-63-01 is a type II RET tyrosine kinase inhibitor (TKI). HG-6-63-01 also inhibits REarranged during Transfection (RET) kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles. HG-6-63-01 impairs phosphorylation and signalling of RET oncogenic mutants. HG-6-63-01 blunts proliferation of RET/C634R and RET/M918T-transformed fibroblasts and of RET mutant thyroid cancer cells, which is promising for research of cancers harboring oncogenic activation of RET.

AD80 (Standard) is the analytical standard of AD80 (HY-101963). This product is intended for research and analytical applications. AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

Amuvatinib (Standard) is the analytical standard of Amuvatinib. This product is intended for research and analytical applications. Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.

Regorafenib (Standard) is the analytical standard of Regorafenib. This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.

GSK3179106 (Standard) is the analytical standard of GSK3179106 (HY-100459). This product is intended for research and analytical applications. GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity.

KBP-7018 is an orally active, tyrosine kinase-selective multi-kinase inhibitor with an IC₅₀ value of 10 nM against c-KIT, 7.6 nM against RET, and 25 nM against human PDGFR. KBP-7018 improves survival rates in a mouse model of pulmonary fibrosis. KBP-7018 can be used in research related to idiopathic pulmonary fibrosis.

Pyrazoloadenine (Standard) is the analytical standard of Pyrazoloadenine. This product is intended for research and analytical applications. Pyrazoloadenine is a potent RET (REarranged during Transfection) lung cancer oncoprotein inhibitor. Pyrazoloadenine shows anticancer activity.

PF 477736 (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

trans-Pralsetinib (Standard) is the analytical standard of trans-Pralsetinib. This product is intended for research and analytical applications. trans-Pralsetinib (trans-BLU-667) is a rearranged during transfection (RET) inhibitor extracted from patent US20170121312A1, Compound Example 129.

TG101209 (Standard) is the analytical standard of TG101209 (HY-10410). This product is intended for research and analytical applications. TG101209 is a selective JAK2 inhibitor with IC₅₀ of 6 nM, less potent to Flt3 and RET with IC₅₀ of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.

FHND5071 is a potent and selective RET kinase inhibitor, FHND5071 can exert antitumor effects by inhibiting RET autophosphorylation. FHND5071 can be used for tumor diseases research.

Lenvatinib (mesylate) (Standard) is the analytical standard of Lenvatinib (mesylate). This product is intended for research and analytical applications. 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.

XMD15-44 is a RET kinase inhibitor.XMD15-44 has a growth-inhibitory effect on RET/C634R and RET/M918T transformed RAT1 cells, with IC₅₀ values of 11.5 nM and 8.3 nM, respectively. XMD15-44 can inhibit RET kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles, reducing cell proliferation.

SYHA1815 is an orally active RET inhibitor (IC₅₀=0.9 nmol/L) with antitumor activity. SYHA1815 is more selective for RET than KDR (IC₅₀=15.9 nmol/L). SYHA1815 arrests the G1 cell cycle and inhibits RET-driven cell proliferation by downregulating c-Myc.