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In vitro: Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells.
In vivo: Early/sustained but not late/acute administration of ARRY-470(LOXO-101) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier
| Cell Experiment | |
|---|---|
| Cell lines | Ba/F3 cells |
| Preparation method | Ba/F3 cells expressing MPRIP-NTRK1 (RIP-TRKA) or EV were lysed after 5 h of treatment with the indicated doses of drugs (ARRY-470; G, gefitinib 1,000 nM) or DMSO control. The cell lysate are used for western bolt analysis. |
| Concentrations | 10, 100, 1000 nM |
| Incubation time | 5 h |
| Animal Experiment | |
|---|---|
| Animal models | Adult male C3H/HeJ mice |
| Formulation | Labrafac;polygly-colyzed glyceride |
| Dosages | 10-100 mg/kg |
| Administration | p.o. |
| Molecular Weight | 526.51 |
| Formula | C21H22F2N6O2.H2O4S |
| CAS Number | 1223405-08-0 |
| Solubility (25°C) | DMSO 50 mg/mL (Need ultrasonic) |
| Storage | 4°C, dry, sealed |
| Related Trk Products |
|---|
| GNF-5837
GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively. |
| GW441756
GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. |
| ANA-12
ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively. |
| 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). |
| Larotrectinib (LOXO-101)
Larotrectinib (LOXO-101) is a potent, ATP competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases. |
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