LOXO-195 free base · Synonyms: LOXO 195 | Selitrectinib

Selitrectinib is an orally available, highly potent, and selective TRK kinase inhibitor.

For research use only. Not for human or veterinary use.

Target Trk Receptor

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

LOXO-195 structure

CAS No.: 2097002-61-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 550.00	BP-02341-100mg	Inquire	Get quote
250 mg	USD 750.00	BP-02341-250mg	In stock	Get quote
500 mg	USD 1,050.00	BP-02341-500mg	In stock	Get quote
1 g	USD 1,450.00	BP-02341-1g	In stock	Get quote
5 g	Inquire	BP-02341-5g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

Selitrectinib (LOXO-195, BAY 2731954) is an orally available, highly potent, and selective TRK kinase inhibitor with low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C.

Biological activity

Selitrectinib (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. Selitrectinib (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, Selitrectinib (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.

Identifiers

SMILES: [H][C@]12CCCN1C1=NC3=C(C=NN3C=C1)C(=O)N[C@H](C)CCC1=NC=C(F)C=C21
InChIKey: OEBIHOVSAMBXIB-SJKOYZFVSA-N

Specifications

MW (average): 380.4187
Formula: C₂₀H₂₁FN₆O
CAS No.: 2097002-61-2
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Drilon A, 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. 2017, 7(9):963-972.

Same target

Search Trk Receptor

Same research area

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