- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|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|
|S8573||Sitravatinib (MGCD516)||<1 mg/mL||100 mg/mL||100 mg/mL|
|S8570||RXDX-106 (CEP-40783)||<1 mg/mL||10 mg/mL||2 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|
|S7669||NPS-1034||<1 mg/mL||100 mg/mL||4 mg/mL|
- TAM Receptor Inhibitors (11)
- New TAM Receptor Products
|Catalog No.||Information||Product Use Citations||Product Validations|
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.
Numbers of clonogenic cells from L3.6pl cells and CSCs＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%.
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).
Cetuximab-resistant cells are sensitive to therapeutic blockade of AXL activity with the AXL TKI R428. Cells were treated with vehicle (-) or indicated doses of R428 for 24 hours before harvesting whole-cell lysate and immunoblotting for the indicated proteins. α-Tubulin was used as a loading control.
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.
Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
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.
a-c Concentration of secreted IL-1β, IL-8 and CCL2 in THP-1 macrophages treated with or without recombinant human IL-37 (rhIL-37) for 3 h, followed by incubation for 1 h with or without Mertk inhibitor and then incubated with lipopolysaccharide (LPS) or MSU separately for a further 18 h; *P < 0.05. d Different dosage of rhIL-37 was given preventively or therapeutically with or without Mertk inhibitor intervention in mice with gouty arthritis, and foot thickness was evaluated; *P < 0.05. e, f Histopathological analysis by H&E staining in a joint from the group treated with rhIL-37 treatment and Mertk inhibitor intervention (×100 original magnification (e) and × 200 original magnification (f); arrow inflammation in soft tissue and joint space.
TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM.
Phosphorylation of Axl was analyzed by Western blotting of whole cell lysates using different antibodies. GAPDH was used as an internal control. H1299 cells were stimulated for 15 min with 400 nM recombinant human Gas6 (rGas6). H1299 cells were treated with or without TP-0903 (0.2 µmol/L) for 24 h.
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.
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.
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.
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.
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.
NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.