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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).
T1995 FedratinibHOT Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
T2070 CEP-32496 CEP-32496 is a highly potent inhibitor of BRAF.
T2094 Danusertib Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may...
T2282 RPI-1 RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor. 
T2358 ENMD-2076 ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
T2620 G-749 G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.
T3065 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
T4053 AST 487 AST 487 is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
T6982 SGI-7079 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 EGF...
T4301 AD80 AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
T5153 Apatinib mesylate Apatinib is an orally bioavailable and specific VEGFR2 inhibitor (IC50: 1 nM). In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.
T5491 GSK3179106 GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM
T7418 BBT594 BBT594(NVP-BBT594) is a potent inhibitor of receptor tyrosine kinase RET,Treatment of cancer.
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-R...
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 suppres...
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).
T6920 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11nM).
T5171 Treprostinil Sodium Treprostinil is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM).
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), ...
T8402 Regorafenib Hydrochloride Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor a...
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).
T10823 cis-Pralsetinib trans-Pralsetinib (trans-BLU-667) is an inhibitor of rearranged during transfection (RET) extracted from patent US20170121312A1 (Compound Example 129).
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,...
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).
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.
CEP-32496
T2070CAS 1188910-76-0
CEP-32496 is a highly potent inhibitor of BRAF.
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...
RPI-1
T2282CAS 269730-03-2
RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor. 
ENMD-2076
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.
G-749
T2620CAS 1457983-28-6
G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.
TG101209
T3065CAS 936091-14-4
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
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.
SGI-7079
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 EGF...
AD80
T4301CAS 1384071-99-1
AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
Apatinib mesylate
T5153CAS 1218779-75-9
Apatinib is an orally bioavailable and specific VEGFR2 inhibitor (IC50: 1 nM). In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.
GSK3179106
T5491CAS 1627856-64-7
GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM
BBT594
T7418CAS 882405-89-2
BBT594(NVP-BBT594) is a potent inhibitor of receptor tyrosine kinase RET,Treatment of cancer.
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-R...
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 suppres...
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).
ON123300
T6920CAS 1357470-29-1
ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11nM).
Treprostinil Sodium
T5171CAS 289480-64-4
Treprostinil is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM).
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), ...
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 a...
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).
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).
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,...