Trk receptor

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
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
S8348 BMS-935177 <1 mg/mL 100 mg/mL 100 mg/mL
S7998 Entrectinib (RXDX-101) <1 mg/mL 100 mg/mL 75 mg/mL
S8573 Sitravatinib (MGCD516) <1 mg/mL 100 mg/mL 100 mg/mL
S8407 PF-06273340 <1 mg/mL 95 mg/mL 1 mg/mL
S8511 Belizatinib (TSR-011) <1 mg/mL 100 mg/mL 100 mg/mL
S7960 Larotrectinib (LOXO-101) sulfate <1 mg/mL 100 mg/mL 100 mg/mL
S7745 ANA-12 <1 mg/mL 37 mg/mL <1 mg/mL
S8319 7,8-Dihydroxyflavone <1 mg/mL 50 mg/mL 1 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1124

BMS-754807

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.

S2891

GW441756

GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2.

S7519

GNF-5837

GNF-5837 is a selective, and orally bioavailable pan-TRK inhibitor for TrkA, and TrkB with IC50 of 8 nM, and 12 nM, respectively.

S8348New

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.

S7998

Entrectinib (RXDX-101)

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.

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.

S8407

PF-06273340

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.

S8511

Belizatinib (TSR-011)

"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). "

S7960

Larotrectinib (LOXO-101) sulfate

Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

S7745

ANA-12

ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively.

S8319

7,8-Dihydroxyflavone

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).