A Trk kinase inhibitor
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LOXO-195

Item No. 27062

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3aR,10R)-5-fluoro-1,2,3,3a,8,9,10,11-octahydro-10-methyl-12H-15,17-ethenopyrazolo[3,4-d]pyrido[2,3-k]pyrrolo[2,1-m][1,3,7]triazacyclotridecin-12-one
CAS Number
2097002-61-2
Synonyms
  • Selitrectinib
Molecular Formula
C20H21FN6O
Formula Weight
380.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12 mg/mlDMSO: 5 mg/mlEthanol: 3 mg/ml
λmax
228, 265 nm
SMILES
O=C(N[C@H](C)CCC1=NC=C(F)C=C1[C@]2([H])N3CCC2)C4=C5N(N=C4)C=CC3=N5
InChi Code
InChI=1S/C20H21FN6O/c1-12-4-5-16-14(9-13(21)10-22-16)17-3-2-7-26(17)18-6-8-27-19(25-18)15(11-23-27)20(28)24-12/h6,8-12,17H,2-5,7H2,1H3,(H,24,28)/t12-,17-/m1/s1
InChi Key
OEBIHOVSAMBXIB-SJKOYZFVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    LOXO-195 is an inhibitor of the receptor tyrosine kinases TrkA and TrkC (IC50s = 0.6 and <2.5 nM, respectively, in kinase assays).1 It also inhibits several Trk kinase mutants, including TrkAG595R, TrkAG667C, TrkCG623R, and TrkCG696A (IC50s = 2, 9.8, 2.3, and <2.5 nM, respectively). LOXO-195 binds to the kinase domain of TrkB with an IC50 value of 1.9 nM. It selectively inhibits proliferation of Trk fusion-positive K12, CUTO-3, and MO-91 cell lines (IC50s = ≤5 nM) over Trk fusion-negative cell lines when used at concentrations up to 10 μM. LOXO-195 (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Drilon, A., Nagasubramanian, R., Blake, J.F., et al. A next-generation TRK kinase inhibitor overcomes acquired resistance to prior TRK kinase inhibition in patients with TRK fusion-positive solid tumors. Cancer Discov. 7(9), 963-972 (2017).