LOXO-101 (ARRY-470, Larotrectinib) | TRK inhibitor | Probechem Biochemicals

Chemical Structure : LOXO-101

CAS No.: 1223403-58-4

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LOXO-101 (Larotrectinib, ARRY470, ARRY-470, LOXO101)

货号: 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.

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10 mg	￥780	In stock
25 mg	￥1280	In stock
50 mg	￥2180	In stock
100 mg	￥3480	In stock
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	428.4352
分子式	C21H22F2N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	DMSO: ≥ 4.6 mg/mL
Chemical Name/SMILES	1-Pyrrolidinecarboxamide, N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, (3S)-

参考文献

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.

LOXO-101 (Larotrectinib, ARRY470, ARRY-470, LOXO101)

生物&药学活性

物理化学性质&存储条件

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LOXO-101 (Larotrectinib, ARRY470, ARRY-470, LOXO101)

生物&药学活性

物理化学性质&存储条件

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