1. Neuronal Signaling
    Protein Tyrosine Kinase/RTK
  2. Trk Receptor
  3. LPM4870108

LPM4870108 

Cat. No.: HY-132229
Handling Instructions

LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity.

For research use only. We do not sell to patients.

LPM4870108 Chemical Structure

LPM4870108 Chemical Structure

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Description

LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity[1][2].

IC50 & Target[1]

TrkC

0.2 nM (IC50)

TrkA

2.4 nM (IC50)

In Vitro

LPM4870108 (compound 10) inhibits the activities of TrkA, TrkB, and TRC with high selectivity at 0.5 μM (kinase activity remaining, <10%) and slightly inhibit the activities of ALK and ROS1 (kinase activity remaining, 10-30%)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LPM4870108 (compound 10) (5-20 mg/kg; p.o. once daily for 21 days) inhibits tumor growth in BaF3-NTRK xenograft tumor models[1].
LPM4870108 (2 mg/kg; a single i.v.) exhibits terminal half-life (t1/2) (male 0.87 h, 2.21 h), the Cl (male 19.3 mL/kg/min, female 8.19 mL/kg/min), and the AUC0-t (male 4191 nM•h, female 10282 nM•h) in rats[1].
LPM4870108 (10 mg/kg; a single p.o.) exhibits oral bioavailability (male 56.0%, female 61.9%), Cmax (male 6384 nM, female 6628 nM) and Tmax (male 0.667 h, female 0.667 h) in rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice bearing 100-200 mm3 BaF3-NTRK tumors[1]
Dosage: 5, 10, 20 mg/kg
Administration: P.o. once daily for 21 days
Result: Showed slight weight loss and all animals survived at the highest dose.
Animal Model: Sprague-Dawley rats (six males and six females)[1]
Dosage: 2 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: I.v.: t1/2 (male 0.87 h, 2.21 h), Cl (male 19.3 mL/kg/min, female 8.19 mL/kg/min), AUC0-t (male 4191 nM•h, female 10282 nM•h).
P.o.: F (male 56.0%, female 61.9%), Cmax (male 6384 nM, female 6628 nM), Tmax (male 0.667 h, female 0.667 h).
Molecular Weight

410.40

Formula

C₂₀H₁₉FN₆O₃

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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LPM4870108
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HY-132229
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