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Apoptosis c-RET

c-RET

The RET proto-oncogene encodes a receptor tyrosine kinase for members of the glial cell line-derived neurotrophic factor (GDNF) family of extracellular signalling molecules. RET loss of function mutations are associated with the development of Hirschsprung's disease,[citation needed] while gain of function mutations are associated with the development of various types of human cancer, including medullary thyroid carcinoma, multiple endocrine neoplasias type 2A and 2B, pheochromocytoma and parathyroid hyperplasia.
Cat No. product name
T1792 RegorafenibHOT Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor (IC50s: 1.5/2.5/4.2/7/13/22 nM for RET/C-RAF/VEGFR2/c-Kit/VEGFR1/PDGFRβ).
T2586 CabozantinibHOT Cabozantinib (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50s: 0.035, 1.3, 4.6, 7 and 11.3 nM).
T1995 FedratinibHOT Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
T1792L Regorafenib monohydrate 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 VEGFR...
T5171 Treprostinil Sodium Treprostinil is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM).
T6982 SGI7079 SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR...
T6132 ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more select...
T6920 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).
T2620 G749 G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.
T2282 RPI1 RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor.
T2094 Danusertib Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may ...
T2358 ENMD2076 ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
T3065 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
T4301 AD80 AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.
T4053 AST 487 AST 487 is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
T5491 GSK3179106 GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM
T22349 CS-2660 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 ...
T7418 BBT594 BBT594(NVP-BBT594) is a potent inhibitor of receptor tyrosine kinase RET,Treatment of cancer.
TQ0059 Ilorasertib Ilorasertib (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 suppress...
TQ0277 Pralsetinib Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RE...
T8222 Selpercatinib Selpercatinib is a tyrosine kinase inhibitor with antineoplastic properties(IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), r...
T8402 Regorafenib Hydrochloride Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor ac...
T8467 RET V804M-IN-1 RET V804M-IN-1 is a wt-RET -selective RETV804M kinase inhibitors(IC50 = 20 nM).
T14928 Agerafenib hydrochloride Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).
T10624 BT-13 BT-13 is a selective agonist of glial cell line-derived neurotrophic factor (GDNF) receptor RET independently of GFLs. BT-13 promotes neurite growth from sensory...
T10823 Cis-Pralsetinib trans-Pralsetinib (trans-BLU-667) is an inhibitor of rearranged during transfection (RET) extracted from patent US20170121312A1 (Compound Example 129).
T10157 Regorafénib N-oxyde (M2) Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, RET, Kit, and Raf-1 (IC50s: 13/4...
T8541 Lenvatinib mesylate Lenvatinib mesylate is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.
T16923 SPP-86 SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling. SPP-86 also inhibits RET-induced estrogen receptorα phosphorylation ...
T16995 TAS05567 TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, ...
T2070 CEP32496 CEP-32496 is a highly potent inhibitor of BRAF.
Regorafenib HOT
T1792CAS 755037-03-7
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor (IC50s: 1.5/2.5/4.2/7/13/22 nM for RET/C-RAF/VEGFR2/c-Kit/VEGFR1/PDGFRβ).
Cabozantinib HOT
T2586CAS 849217-68-1
Cabozantinib (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50s: 0.035, 1.3, 4.6, 7 and 11.3 nM).
Fedratinib HOT
T1995CAS 936091-26-8
Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
Regorafenib monohydrate
T1792LCAS 1019206-88-2
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 VEGFR...
Treprostinil Sodium
T5171CAS 289480-64-4
Treprostinil is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM).
SGI7079
T6982CAS 1239875-86-5
SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR...
ENMD-2076 L-(+)-Tartaric acid
T6132CAS 1291074-87-7
ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more select...
ON123300
T6920CAS 1357470-29-1
ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).
G749
T2620CAS 1457983-28-6
G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.
RPI1
T2282CAS 269730-03-2
RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor.
Danusertib
T2094CAS 827318-97-8
Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may ...
ENMD2076
T2358CAS 934353-76-1
ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
TG101209
T3065CAS 936091-14-4
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
AD80
T4301CAS 1384071-99-1
AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.
AST 487
T4053CAS 630124-46-8
AST 487 is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
GSK3179106
T5491CAS 1627856-64-7
GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM
CS-2660
T22349CAS 951151-97-6
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 ...
BBT594
T7418CAS 882405-89-2
BBT594(NVP-BBT594) is a potent inhibitor of receptor tyrosine kinase RET,Treatment of cancer.
Ilorasertib
TQ0059CAS 1227939-82-3
Ilorasertib (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 suppress...
Pralsetinib
TQ0277CAS 2097132-94-8
Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RE...
Selpercatinib
T8222CAS 2152628-33-4
Selpercatinib is a tyrosine kinase inhibitor with antineoplastic properties(IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), r...
Regorafenib Hydrochloride
T8402CAS 835621-07-3
Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor ac...
RET V804M-IN-1
T8467CAS 2414909-94-5
RET V804M-IN-1 is a wt-RET -selective RETV804M kinase inhibitors(IC50 = 20 nM).
Agerafenib hydrochloride
T14928CAS 1227678-26-3
Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).
BT-13
T10624CAS 924537-98-4
BT-13 is a selective agonist of glial cell line-derived neurotrophic factor (GDNF) receptor RET independently of GFLs. BT-13 promotes neurite growth from sensory...
cis-Pralsetinib
T10823CAS 2097132-93-7
trans-Pralsetinib (trans-BLU-667) is an inhibitor of rearranged during transfection (RET) extracted from patent US20170121312A1 (Compound Example 129).
Regorafénib N-oxyde (M2)
T10157CAS 835621-11-9
Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, RET, Kit, and Raf-1 (IC50s: 13/4...
Lenvatinib mesylate
T8541CAS 857890-39-2
Lenvatinib mesylate is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.
SPP-86
T16923CAS 1357349-91-7
SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling. SPP-86 also inhibits RET-induced estrogen receptorα phosphorylation ...
TAS05567
T16995CAS 1429038-15-2
TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, ...
CEP32496
T2070CAS 1188910-76-0
CEP-32496 is a highly potent inhibitor of BRAF.