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LOXO-101 sulfate

Chemical Structure : LOXO-101 sulfate

CAS No.: 1223405-08-0

LOXO-101 sulfate (LOXO101 sulfate;LOXO 101 sulfate;Larotrectinib sulfate)

Catalog No.: PC-43266Not For Human Use, Lab Use Only.

LOXO-101 (ARRY-470, Larotrectinib) is potent, selective pan-TRK inhibitor with cellular IC50 of 2-20 nM against TRKA, TRKB, and TRKC kinases.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LOXO-101 (ARRY-470, Larotrectinib) is potent, selective pan-TRK inhibitor with cellular IC50 of 2-20 nM against TRKA, TRKB, and TRKC kinases; demonstrates excellent selectivity against a panel of 226 non-TRK kinases with one exception (TNK2 IC50=576 nM); inhibits fusion oncoprotein and cellular proliferation in TRK-fusion-bearing human-derived cancer cell lines; markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone; inhibits tumor growth in vivo in TRK fusion-positive cancer models.

Blood Cancer

Phase 2 Clinical

Physicochemical Properties

M.Wt 526.5137
Formula C21H24F2N6O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO

Chemical Name/SMILES

1-Pyrrolidinecarboxamide, N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, (3S)-, sulfate (1:1)

References

1. Doebele RC, et al. Cancer Discov. 2015 Oct;5(10):1049-57.

2. Ghilardi JR, et al. Mol Pain. 2010 Dec 7;6:87.

3. Vaishnavi A, et al. Nat Med. 2013 Nov;19(11):1469-1472.

4. Drilon A, et al. N Engl J Med. 2018 Feb 22;378(8):731-739.

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