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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Trk Receptor-LOXO-101 sulfate
LOXO-101 sulfate

Chemical Structure : LOXO-101 sulfate

CAS No.: 1223405-08-0

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LOXO-101 sulfate (ARRY-470 sulfate, Larotrectinib sulfate)

货号: PC-43266Not For Human Use, Lab Use Only.

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

规格 价格 库存 数量
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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LOXO-101 (ARRY-470, Larotrectinib) sulfate is potent, selective pan-TRK inhibitor with cellular IC50 of 2-20 nM against TRKA, TRKB, and TRKC kinases.
LOXO-101 (ARRY-470, Larotrectinib) 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 526.5137
分子式 C21H24F2N6O6S
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

10 mM in PBS
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)

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.

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