- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S1124||BMS-754807||<1 mg/mL||92 mg/mL||92 mg/mL|
|S2891||GW441756||<1 mg/mL||25 mg/mL||<1 mg/mL|
|S7519||GNF-5837||<1 mg/mL||100 mg/mL||9 mg/mL|
|S7998||Entrectinib (RXDX-101)||<1 mg/mL||100 mg/mL||75 mg/mL|
|S7745||ANA-12||<1 mg/mL||37 mg/mL||<1 mg/mL|
|S8511||Belizatinib (TSR-011)||<1 mg/mL||100 mg/mL||100 mg/mL|
|S8407||PF-06273340||<1 mg/mL||95 mg/mL||1 mg/mL|
|S8583||TPX-0005||<1 mg/mL||70 mg/mL||10 mg/mL|
|S8573||Sitravatinib (MGCD516)||<1 mg/mL||100 mg/mL||100 mg/mL|
|S8319||7,8-Dihydroxyflavone||<1 mg/mL||50 mg/mL||1 mg/mL|
|S7960||Larotrectinib (LOXO-101) sulfate||<1 mg/mL||100 mg/mL||100 mg/mL|
- Trk receptor Inhibitors (11)
- New Trk receptor Products
|Catalog No.||Information||Product Use Citations||Product Validations|
BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.
GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2.
Effect of TrkA inhibitorGW441756 on vorinostat andNGFmediated ERK phosphorylation. A)NS-1 cellswere treatedwith vorinostat (1 and 2.5 μM) andNGF (2.5 ng/mL)with and without GW441756 (1 μM) for 3 h. The blots were probed with anti-pERK.1/2 antibody. Vorinostat mediated activation of ERK1/2 phosphorylation (pErk) was abolished in presence of GW441756. Total ERK levels were checked using ERK 1/2 antibody. B) Bar graph represents the densitometric analysis of immunoblots. X axis represents treatments and Y axis represents the ratio of absolute relative density of pERK to the total ERK. The data sets are the mean ± SE of two biological replicates from two independent experiments (values compared to control vs vorinostat 1 μM and 2.5 μM, vorinostat 1 μM and 2.5 μM Vs GW441756 + vorinostat 1 and 2.5 μM respectively). *P < 0.05, **P < 0.001, ***P < 0.0001 indicate significant differences and ns indicates non-significant difference.
GNF-5837 is a selective, and orally bioavailable pan-TRK inhibitor for TrkA, and TrkB with IC50 of 8 nM, and 12 nM, respectively.
Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.
ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively.
"Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). "
PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.
TPX-0005 is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).
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.
7,8-Dihydroxyflavone acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF).
Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).