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LOXO-195

Cat. No. M9107
LOXO-195 Structure
Synonym:

LOXO195

Size Price Availability Quantity
2mg USD 450 In stock
5mg USD 650 In stock
10mg USD 990 In stock
25mg USD 1990 In stock
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Quality Control
Biological Activity

LOXO-195 is a potent and selective, next-generation TRK inhibitor, with IC50 values of 0.6±0.1 nM, <2.5 nM for TRKA and TRKC, respectively. LOXO-195 achieves low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, with IC50s ranging from 2.0-9.8 nM. LOXO-195 demonstrates potent inhibition of cell proliferation in TRK fusion-containing KM12, CUTO-3, and MO-91 cell lines (IC50≤5 nM).

In diverse TRK fusion mouse models, LOXO-195 also causes inhibition of tumor growth relative to vehicle at all doses in four TRKA-dependent tumor models, superior to first generation TRK inhibitors, without significant toxicity.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 380.42
Formula C20H21FN6O
CAS Number 2097002-61-2
Purity 99.67%
Solubility DMSO: ≥ 55 mg/mL (Need ultrasonic)
Storage at -20°C
References

A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors.
Drilon A, et al. Cancer Discov. 2017 Sep;7(9):963-972. PMID: 28578312.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LOXO-195, LOXO195 supplier, Trk, inhibitors

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