S0377 |
CS-2660 (JNJ-38158471)
|
CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3. |
|
|
S1107 |
Danusertib (PHA-739358)
|
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2. |
-
Cancers (Basel), 2021, 13(6)1205
-
Life Sci Alliance, 2021, 4(8)e202101019
-
Mol Cell, 2020, 80(6):1104-1122.e9
|
|
S1164 |
Lenvatinib (E7080)
|
Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3. |
-
Clin Transl Med, 2022, 12(1):e662
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Nature, 2021, 595(7869):730-734
|
|
S1178 |
Regorafenib (BAY 73-4506)
|
Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy. |
-
Cancer Cell, 2022, S1535-6108(21)00662-0
-
Cell Rep, 2022, 38(10):110490
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S1244 |
Amuvatinib (MP-470)
|
Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
mBio, 2021, 12(6):e0322821
-
Hum Cell, 2021, 34(6):1911-1918
|
|
S2692 |
TG101209
|
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET (c-RET) with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations. |
-
EBioMedicine, 2022, 78:103963
-
Sci Rep, 2022, 12(1):7
-
Cell Death Discov, 2021, 7(1):268
|
|
S2736 |
Fedratinib (TG101348)
|
Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2. |
-
J Immunother Cancer, 2022, 10(1)e003766
-
Int J Mol Sci, 2022, 23(4)2019
-
Sci Rep, 2022, 12(1):7
|
|
S4001 |
Cabozantinib malate (XL184)
|
Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis. |
-
Cancer Res, 2022, canres.1397.2021
-
Cancers (Basel), 2022, 14(6)1378
-
Endocr Relat Cancer, 2022, ERC-21-0258
|
|
S4947 |
Regorafenib Hydrochloride
|
Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. |
-
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
-
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
-
Front Oncol, 2021, 11:796839
|
|
S5077 |
Regorafenib (BAY-734506) Monohydrate
|
Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) 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 VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. |
-
Pharmazie, 2022, 77(2):54-58
-
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
-
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
|
|
S5240 |
Lenvatinib (E7080) Mesylate
|
Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity. |
-
Clin Transl Med, 2022, 12(1):e662
-
Pharmazie, 2022, 77(2):54-58
-
J Immunother Cancer, 2021, 9(6)e002305
|
|
S5248 |
Apatinib
|
Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis. |
-
Front Oncol, 2021, 11:739139
-
Biochem Biophys Res Commun, 2021, 586:177-184
-
Cells, 2020, 9(6):E1452
|
|
S6520 |
WHI-P180
|
WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively. |
|
|
S6662 |
AST-487 (NVP-AST487)
|
AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. |
-
Nat Commun, 2020, 21;11(1):1924
|
|
S8015 |
Agerafenib (RXDX-105)
|
Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. |
-
Mol Pharmacol, 2021, 99(6):435-447
-
Dis Model Mech, 2020, dmm.047779
-
Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
|
|
S8161 |
ON123300
|
ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively. |
-
J Cell Sci, 2021, jcs.258685
-
Molecules, 2020, 8;25(9) pii: E2220
|
|
S8189 |
BAW2881 (NVP-BAW2881)
|
BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations. |
-
JCI Insight, 2021, 143285
-
J Cell Biochem, 2019, 120(4):5583-5596
|
|
S8401 |
Erdafitinib (JNJ-42756493)
|
Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. |
-
JCI Insight, 2022, 7(7)e154824
-
Oncoimmunology, 2022, 11(1):2021619
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S8518 |
AD80
|
AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM. |
-
Mol Cancer Res, 2020, 1176-1188
-
Mol Cancer Res, 2020, 18(8):1176-1188
-
Mol Cancer Res, 2020, 27;molcanres.1245.2019
|
|
S8696 |
2-D08
|
2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays. |
-
Nat Commun, 2021, 12(1):4794
-
Cancers (Basel), 2021, 13(14)3475
-
Cancer Sci, 2021, 112(10):4075-4086
|
|
S8716 |
Pralsetinib (BLU-667)
|
Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T). |
-
Mol Cancer Res, 2020, 18(8):1176-1188
-
Mol Cancer Res, 2020, 1176-1188
-
Mol Cancer Res, 2020, 27;molcanres.1245.2019
|
|
S8781 |
Selpercatinib (LOXO-292)
|
Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET (c-RET) inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively. |
-
Cancer Res, 2022, canres.1397.2021
|
|
S8821 |
GSK3179106
|
GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET (c-RET) kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo. |
|
|
S9826New |
TPX-0046
|
TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.
|
|
|
S0377 |
CS-2660 (JNJ-38158471)
|
CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3. |
|
|
S1107 |
Danusertib (PHA-739358)
|
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2. |
- Cancers (Basel), 2021, 13(6)1205
- Life Sci Alliance, 2021, 4(8)e202101019
- Mol Cell, 2020, 80(6):1104-1122.e9
|
|
S1164 |
Lenvatinib (E7080)
|
Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3. |
- Clin Transl Med, 2022, 12(1):e662
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Nature, 2021, 595(7869):730-734
|
|
S1178 |
Regorafenib (BAY 73-4506)
|
Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy. |
- Cancer Cell, 2022, S1535-6108(21)00662-0
- Cell Rep, 2022, 38(10):110490
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S1244 |
Amuvatinib (MP-470)
|
Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- mBio, 2021, 12(6):e0322821
- Hum Cell, 2021, 34(6):1911-1918
|
|
S2692 |
TG101209
|
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET (c-RET) with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations. |
- EBioMedicine, 2022, 78:103963
- Sci Rep, 2022, 12(1):7
- Cell Death Discov, 2021, 7(1):268
|
|
S2736 |
Fedratinib (TG101348)
|
Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2. |
- J Immunother Cancer, 2022, 10(1)e003766
- Int J Mol Sci, 2022, 23(4)2019
- Sci Rep, 2022, 12(1):7
|
|
S4001 |
Cabozantinib malate (XL184)
|
Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis. |
- Cancer Res, 2022, canres.1397.2021
- Cancers (Basel), 2022, 14(6)1378
- Endocr Relat Cancer, 2022, ERC-21-0258
|
|
S4947 |
Regorafenib Hydrochloride
|
Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. |
- ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
- Front Oncol, 2021, 11:796839
|
|
S5077 |
Regorafenib (BAY-734506) Monohydrate
|
Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) 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 VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. |
- Pharmazie, 2022, 77(2):54-58
- ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
|
|
S5240 |
Lenvatinib (E7080) Mesylate
|
Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity. |
- Clin Transl Med, 2022, 12(1):e662
- Pharmazie, 2022, 77(2):54-58
- J Immunother Cancer, 2021, 9(6)e002305
|
|
S5248 |
Apatinib
|
Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis. |
- Front Oncol, 2021, 11:739139
- Biochem Biophys Res Commun, 2021, 586:177-184
- Cells, 2020, 9(6):E1452
|
|
S6520 |
WHI-P180
|
WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively. |
|
|
S6662 |
AST-487 (NVP-AST487)
|
AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. |
- Nat Commun, 2020, 21;11(1):1924
|
|
S8015 |
Agerafenib (RXDX-105)
|
Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. |
- Mol Pharmacol, 2021, 99(6):435-447
- Dis Model Mech, 2020, dmm.047779
- Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
|
|
S8161 |
ON123300
|
ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively. |
- J Cell Sci, 2021, jcs.258685
- Molecules, 2020, 8;25(9) pii: E2220
|
|
S8189 |
BAW2881 (NVP-BAW2881)
|
BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations. |
- JCI Insight, 2021, 143285
- J Cell Biochem, 2019, 120(4):5583-5596
|
|
S8401 |
Erdafitinib (JNJ-42756493)
|
Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. |
- JCI Insight, 2022, 7(7)e154824
- Oncoimmunology, 2022, 11(1):2021619
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S8518 |
AD80
|
AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM. |
- Mol Cancer Res, 2020, 1176-1188
- Mol Cancer Res, 2020, 18(8):1176-1188
- Mol Cancer Res, 2020, 27;molcanres.1245.2019
|
|
S8696 |
2-D08
|
2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays. |
- Nat Commun, 2021, 12(1):4794
- Cancers (Basel), 2021, 13(14)3475
- Cancer Sci, 2021, 112(10):4075-4086
|
|
S8716 |
Pralsetinib (BLU-667)
|
Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T). |
- Mol Cancer Res, 2020, 18(8):1176-1188
- Mol Cancer Res, 2020, 1176-1188
- Mol Cancer Res, 2020, 27;molcanres.1245.2019
|
|
S8781 |
Selpercatinib (LOXO-292)
|
Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET (c-RET) inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively. |
- Cancer Res, 2022, canres.1397.2021
|
|
S8821 |
GSK3179106
|
GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET (c-RET) kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo. |
|
|
S9826New |
TPX-0046
|
TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.
|
|
|