RET
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RET (REarranged during Transfection) is a receptor protein tyrosine kinase, which activates multiple signal transduction pathways. RET protein is composed of three domains: an extracellular ligand-binding domain, a transmembrane domain, and a cytoplasmic tyrosine kinase domain. The RET receptor tyrosine kinase (RTK) regulates key aspects of cellular proliferation and survival by regulating the activity of the mitogen- activated protein kinase (MAPK) and PI3K/Akt signaling pathways. RET also interacts directly with other kinases such as the epidermal growth factor receptor (EGFR) and hepatocyte growth factor receptor (MET) and the focal adhesion kinase (FAK). Furthermore, BRAF and p38MAPK are downstream targets of RET. Kinase inhibitors that simultaneously inhibit RET and its downstream targets.
RET tyrosine kinase receptor presents an attractive therapeutic target for the treatment of certain cancer subsets. Deregulated RET activity has been identified as a causative factor in the development, progression and response to therapy of thyroid carcinoma. Elevated RET expression has been associated with the development of endocrine resistance in human breast cancer.
Products Related to RET(32)
- GC10111RegorafenibCAS: 755037-03-7Purity: >99.00%
Regorafenib is an orally active multi-kinase inhibitor with IC 50 values of 13/4.2/46, 22, 7, 1.5 and 2.5nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
- GC14292Apatinib MesylateCAS: 811803-05-1Purity: >98.00%
Apatinib Mesylate blocks the downstream signal transduction of VEGF pathway to inhibit neovascularization.
- GC15454Lenvatinib (E7080)CAS: 417716-92-8Purity: >99.50%
E7080, known as lenvatinib, is an oral multitargeted tyrosine kinase inhibitor including VEGF, FGF and SCF receptors that has been shown to improve the survival rate of patients with radioiodine-refractory thyroid cancer.
- GC31780Pralsetinib (Blu667)CAS: 2097132-94-8Purity: >98.50%
Pralsetinib (Blu667) is a selective inhibitor of the rearranged during transfection (RET) kinase, indicated for the treatment of certain RET-altered positive tumors.
- GC33362Amuvatinib hydrochloride (MP470 hydrochloride)CAS: 1055986-67-8Purity: >98%
Amuvatinib hydrochloride (MP470 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. Amuvatinib hydrochloride (MP470 hydrochloride) (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
- GC34159Ilorasertib (ABT-348)CAS: 1227939-82-3Purity: >98%
Ilorasertib (ABT-348) (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib (ABT-348) also is a potent VEGF, PDGF inhibitor. Ilorasertib (ABT-348) has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
- GC34809SPP-86CAS: 1357349-91-7Purity: >99.50%
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
- GC37933WHI-P180 hydrochlorideCAS: 153437-55-9Purity: >98%
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.
- GC38519Ilorasertib hydrochlorideCAS: 1847485-91-9Purity: >98.50%
Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
- GC49686N-desmethyl Regorafenib N-oxideCAS: 835621-12-0Purity: >90.00%
An active metabolite of regorafenib
- GC64340ZeteletinibCAS: 2216753-97-6Purity: >98%
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC10035 | TG101209 | 936091-14-4 | >99.50% | |
An inhibitor of JAK2, FLT3, RET, and JAK3 | ||||
| GC10111 | Regorafenib | 755037-03-7 | >99.00% | |
Regorafenib is an orally active multi-kinase inhibitor with IC 50 values of 13/4.2/46, 22, 7, 1.5 and 2.5nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. | ||||
| GC10914 | AST 487 | 630124-46-8 | >99.00% | |
A multi-kinase inhibitor | ||||
| GC14292 | Apatinib Mesylate | 811803-05-1 | >98.00% | |
Apatinib Mesylate blocks the downstream signal transduction of VEGF pathway to inhibit neovascularization. | ||||
| GC14534 | Regorafenib monohydrate | 1019206-88-2 | >99.50% | |
A multi-kinase inhibitor | ||||
| GC14606 | Regorafenib hydrochloride | 835621-07-3 | >99.50% | |
A multi-kinase inhibitor | ||||
| GC15454 | Lenvatinib (E7080) | 417716-92-8 | >99.50% | |
E7080, known as lenvatinib, is an oral multitargeted tyrosine kinase inhibitor including VEGF, FGF and SCF receptors that has been shown to improve the survival rate of patients with radioiodine-refractory thyroid cancer. | ||||
| GC16391 | Amuvatinib (MP-470, HPK 56) | 850879-09-3 | >98.00% | |
A multi-targeted RTK inhibitor | ||||
| GC18492 | GSK3179106 | 1627856-64-7 | >99.00% | |
A RET kinase inhibitor | ||||
| GC19062 | BBT594 | 882405-89-2 | >99.50% | |
BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment. | ||||
| GC31780 | Pralsetinib (Blu667) | 2097132-94-8 | >98.50% | |
Pralsetinib (Blu667) is a selective inhibitor of the rearranged during transfection (RET) kinase, indicated for the treatment of certain RET-altered positive tumors. | ||||
| GC32797 | AD80 | 1384071-99-1 | >99.50% | |
AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity. | ||||
| GC33192 | Selpercatinib | 2152628-33-4 | >98% | |
A RET kinase inhibitor | ||||
| GC33362 | Amuvatinib hydrochloride (MP470 hydrochloride) | 1055986-67-8 | >98% | |
Amuvatinib hydrochloride (MP470 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. Amuvatinib hydrochloride (MP470 hydrochloride) (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity. | ||||
| GC34159 | Ilorasertib (ABT-348) | 1227939-82-3 | >98% | |
Ilorasertib (ABT-348) (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib (ABT-348) also is a potent VEGF, PDGF inhibitor. Ilorasertib (ABT-348) has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). | ||||
| GC34509 | BT-13 | 924537-98-4 | >99.50% | |
BT-13 is a potent and selective glial cell line-derived neurotrophic factor (GDNF) receptor RET agonist independently of GFLs, promoting neurite growth from sensory neurons in vitro and attenuates experimental neuropathy in the Rat. | ||||
| GC34809 | SPP-86 | 1357349-91-7 | >99.50% | |
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells. | ||||
| GC36438 | Lenvatinib mesylate | 857890-39-2 | >99.00% | |
An inhibitor of VEGFR2 and VEGFR3 | ||||
| GC37047 | Pz-1 | 1800505-64-9 | >99.00% | |
Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases. | ||||
| GC37933 | WHI-P180 hydrochloride | 153437-55-9 | >98% | |
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. | ||||
| GC38519 | Ilorasertib hydrochloride | 1847485-91-9 | >98.50% | |
Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). | ||||
| GC49686 | N-desmethyl Regorafenib N-oxide | 835621-12-0 | >90.00% | |
An active metabolite of regorafenib | ||||
| GC60592 | APS6-45 | 2188236-41-9 | >99.50% | |
APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity. | ||||
| GC64340 | Zeteletinib | 2216753-97-6 | >98% | |
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity. | ||||
