LOXO101 free base · Synonyms: LOXO-101 | Larotrectinib

Larotrectinib is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases.

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

Target Trk Receptor Apoptosis

Research area Cancer

Purity 98.72% Stock Inquire

Data Sheet SDS COA

LOXO101 structure

CAS No.: 1223403-58-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
200 mg	USD 500.00	BP-02342-200mg	In stock	Get quote
500 mg	USD 650.00	BP-02342-500mg	In stock	Get quote
1 g	USD 849.00	BP-02342-1g	In stock	Get quote
5 g	USD 2,250.00	BP-02342-5g	In stock	Get quote
10 g	Inquire	BP-02342-10g	In stock	Inquire

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Description

Larotrectinib (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.

Biological activity

In vitro: Larotrectinib (LOXO-101) was evaluated for off-target kinase enzyme inhibition against a panel of 226 non-TRK kinases at a compound concentration of 1,000 nM and ATP concentrations near the Km for each enzyme. LOXO-101 demonstrated greater than 50% inhibition for only one non-TRK kinase (TNK2 IC50 = 576 nM). In vivo: A single dose (30 mg/kg) of LOXO-101 reduced tyrosine phosphorylation of TRKA and downstream signal transduction (pERK) in the tumor >80%. LOXO-101 was well tolerated up to 200 mg/kg/day for 14 d in this model.

Identifiers

SMILES: O[C@H]1CCN(C1)C(=O)NC1=C2N=C(C=CN2N=C1)N1CCC[C@@H]1C1=CC(F)=CC=C1F
InChIKey: NYNZQNWKBKUAII-KBXCAEBGSA-N

Specifications

MW (average): 428.4352
Formula: C₂₁H₂₂F₂N₆O₂
CAS No.: 1223403-58-4
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]. Ghilardi JR, et al. Administration of a tropomyosin receptor kinase inhibitor attenuates sarcoma-induced nerve sprouting, neuroma formation and bone cancer pain. Mol Pain. 2010, 6:87.

[2]. Vaishnavi A, et al. Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer. Nat Med. 2013, 19(11):1469-72.

Same target

Search Trk Receptor

Same research area

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