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Chemical Structure : LOXO-101
CAS No.: 1223403-58-4
Catalog No.: PC-43265Not 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $88 | In stock | |
| 25 mg | $148 | In stock | |
| 50 mg | $238 | In stock | |
| 100 mg | Get quote |
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LOXO-101 (ARRY-470, Larotrectinib) is potent, selective pan-TRK inhibitor with cellular IC50 of 2-20 nM against TRKA, TRKB, and TRKC kinases.
LOXO-101 demonstrates excellent selectivity against a panel of 226 non-TRK kinases with one exception (TNK2 IC50=576 nM.
LOXO-101 inhibits fusion oncoprotein and cellular proliferation in TRK-fusion-bearing human-derived cancer cell lines.
LOXO-101 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.
LOXO-101 inhibits tumor growth in vivo in TRK fusion-positive cancer models.
| M.Wt | 428.4352 | |
| Formula | C21H22F2N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 4.6 mg/mL |
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| Chemical Name/SMILES |
1-Pyrrolidinecarboxamide, N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, (3S)- |
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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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