TAM Receptor

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1561 BMS-777607 <1 mg/mL 47 mg/mL <1 mg/mL
S2841 R428 (BGB324) <1 mg/mL 6 mg/mL <1 mg/mL
S4001 Cabozantinib malate (XL184) <1 mg/mL 100 mg/mL <1 mg/mL
S7342 UNC2250 <1 mg/mL 2 mg/mL <1 mg/mL
S7846 TP-0903 <1 mg/mL 3 mg/mL 1 mg/mL
S8696 2-D08 <1 mg/mL 54 mg/mL <1 mg/mL
S7576 UNC2025 100 mg/mL 25 mg/mL 8 mg/mL
S7638 LDC1267 <1 mg/mL 100 mg/mL 2 mg/mL
S7325 UNC2881 <1 mg/mL 92 mg/mL 5 mg/mL
S8570 RXDX-106 (CEP-40783) <1 mg/mL 10 mg/mL 2 mg/mL
S8404 S49076 <1 mg/mL 87 mg/mL <1 mg/mL
S8573 Sitravatinib (MGCD516) <1 mg/mL 100 mg/mL 100 mg/mL
S7754 Gilteritinib (ASP2215) <1 mg/mL 100 mg/mL 85 mg/mL
S7669 NPS-1034 <1 mg/mL 100 mg/mL 4 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1561

BMS-777607

BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases. Phase 1/2.

S2841

R428 (BGB324)

R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

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, 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.

S7342

UNC2250

UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.

S7846

TP-0903

TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM.

S8696New

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.

S7576

UNC2025

UNC2025 is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.

S7638

LDC1267

LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.

S7325

UNC2881

UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively.

S8570

RXDX-106 (CEP-40783)

RXDX-106 (CEP-40783) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/MET inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.

S8404

S49076

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.

S8573

Sitravatinib (MGCD516)

Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.

S7754

Gilteritinib (ASP2215)

Gilteritinib(ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).

S7669

NPS-1034

NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.