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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Trk Receptor-Entrectinib
Entrectinib

Chemical Structure : Entrectinib

CAS No.: 1108743-60-7

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Entrectinib (NMS-E628, RXDX-101, NMS-01191372, RXDX101)

货号: PC-43144Not For Human Use, Lab Use Only.

Entrectinib (NMS-E628, RXDX-101, NMS-01191372) is a potent, ATP-competitive, orally available pan-TRK, ROS1 and ALK inhibitor with IC50 of 1/3/5/12/7 nM for TRKA/TRKB/TRKC/ALK/ROS1, respectively.

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25 mg ￥1480 In stock
50 mg ￥2380 In stock
100 mg ￥3880 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

Entrectinib (NMS-E628, RXDX-101, NMS-01191372) is a potent, ATP-competitive, orally available pan-TRK, ROS1 and ALK inhibitor with IC50 of 1/3/5/12/7 nM for TRKA/TRKB/TRKC/ALK/ROS1, respectively.
Entrectinib (NMS-E628, RXDX-101, NMS-01191372) exhibits high antiproliferative activity against colorectal carcinoma cell line KM12 with IC50 of 17 nM, abolishes autophosphorylation of TPM3-TRKA, concomitant with complete inhibition of the phosphorylation of PLCγ1, AKT, and MAPK,
Entrectinib (NMS-E628, RXDX-101, NMS-01191372) induces regression in relevant human xenograft tumors, including the TRKA-dependent colorectal carcinoma KM12, ROS1-driven tumors, and several ALK-dependent models.

物理化学性质&存储条件

分子量 560.6375
分子式 C31H34F2N6O2
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: ≥ 31 mg/mL
Chemical Name/SMILES

Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-

参考文献

1. Menichincheri M, et al. J Med Chem. 2016 Apr 14;59(7):3392-408.

2. Ardini E, et al. Mol Cancer Ther. 2016 Apr;15(4):628-39.

3. Rolfo C, et al. Expert Opin Investig Drugs. 2015;24(11):1493-500.

4. Russo M, et al. Cancer Discov. 2016 Jan;6(1):36-44.

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