c-RET

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S1178	Regorafenib (BAY 73-4506)	<1 mg/mL	97 mg/mL	<1 mg/mL
S1107	Danusertib (PHA-739358)	<1 mg/mL	95 mg/mL	<1 mg/mL
S2692	TG101209	<1 mg/mL	102 mg/mL	<1 mg/mL
S8189	BAW2881 (NVP-BAW2881)	<1 mg/mL	84 mg/mL	20 mg/mL
S5248	Apatinib	<1 mg/mL	79 mg/mL	10 mg/mL
S5077	Regorafenib Monohydrate	-1 mg/mL	100 mg/mL	-1 mg/mL
S8696	2-D08	<1 mg/mL	54 mg/mL	<1 mg/mL
S8348	BMS-935177	<1 mg/mL	100 mg/mL	100 mg/mL
S8518	AD80	<1 mg/mL	94 mg/mL	94 mg/mL

c-RET Products

All (9) c-RET Inhibitors (9) New c-RET Products

Catalog No.	Information	Product Use Citations	Product Validations
S1178	Regorafenib (BAY 73-4506) Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, 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.	Gastroenterology, 2017, 153(4):1082-1095 Clin Cancer Res, 2014, 20(22):5768-76 Proc Natl Acad Sci USA, 2015, 112(6):1839-44	Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05
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. Phase 2.	Leukemia, 2018, 10.1038/s41375-018-0102-4 Leukemia, 2013, 27(3):560-8 Cancer Res, 2014, 74(20):5878-90	c, Upper panel: viable cell number of FLT3-ITD-positive AML patient samples incubated with vandetanib, danusertib, or DMSO for 7 days in methylcellulose. The mean ± SD of duplicates is shown. Lower panel: viability and proliferation of mutant FLT3-positive AML cell lines and one AML patient sample treated with vandetanib and crenolanib alone or in combination for 3 days. The calculated additive effects of both inhibitors according to the Bliss Independence model are indicated by the dashed lines. The mean ± SD of four (cell lines) or two (patient sample) independent experiments is shown. P-values were calculated using one-way ANOVA followed by Dunnett’s test for multiple comparisons. P ≤ 0.05; P ≤ 0.01; **P ≤ 0.001.
S2692	TG101209 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 in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.	Leukemia, 2014, 28(7):1519-28 Cancer Lett, 2013, 341(2):224-30 ACS Chem Biol, 2014, 9(5):1160-71	EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (,P < 0.05; , P < 0.01; **, P < 0.001; NS, nonsignificant).
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 at 45-72 nM concentrations.
S5248^New	Apatinib Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively.
S5077^New	Regorafenib Monohydrate Regorafenib 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, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.
S8696^New	2-D08 2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, 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.
S8348^New	BMS-935177 BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective.
S8518	AD80 AD80, a multikinase inhibitor, shows strong activity against human 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.

Catalog No.	Information	Product Use Citations	Product Validations
S1178	Regorafenib (BAY 73-4506) Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, 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.	Gastroenterology, 2017, 153(4):1082-1095 Clin Cancer Res, 2014, 20(22):5768-76 Proc Natl Acad Sci USA, 2015, 112(6):1839-44	Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05
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. Phase 2.	Leukemia, 2018, 10.1038/s41375-018-0102-4 Leukemia, 2013, 27(3):560-8 Cancer Res, 2014, 74(20):5878-90	c, Upper panel: viable cell number of FLT3-ITD-positive AML patient samples incubated with vandetanib, danusertib, or DMSO for 7 days in methylcellulose. The mean ± SD of duplicates is shown. Lower panel: viability and proliferation of mutant FLT3-positive AML cell lines and one AML patient sample treated with vandetanib and crenolanib alone or in combination for 3 days. The calculated additive effects of both inhibitors according to the Bliss Independence model are indicated by the dashed lines. The mean ± SD of four (cell lines) or two (patient sample) independent experiments is shown. P-values were calculated using one-way ANOVA followed by Dunnett’s test for multiple comparisons. P ≤ 0.05; P ≤ 0.01; **P ≤ 0.001.
S2692	TG101209 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 in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.	Leukemia, 2014, 28(7):1519-28 Cancer Lett, 2013, 341(2):224-30 ACS Chem Biol, 2014, 9(5):1160-71	EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (,P < 0.05; , P < 0.01; **, P < 0.001; NS, nonsignificant).
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 at 45-72 nM concentrations.
S5248^New	Apatinib Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively.
S5077^New	Regorafenib Monohydrate Regorafenib 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, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.
S8696^New	2-D08 2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, 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.
S8348^New	BMS-935177 BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective.
S8518	AD80 AD80, a multikinase inhibitor, shows strong activity against human 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.

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