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Chemical Structure : Entrectinib
CAS No.: 1108743-60-7
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $78 | In stock | |
| 25 mg | $218 | In stock | |
| 100 mg | $598 | In stock | |
| 500 mg | Get quote |
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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; 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; induces regression in relevant human xenograft tumors, including the TRKA-dependent colorectal carcinoma KM12, ROS1-driven tumors, and several ALK-dependent models.
Lung Cancer
Phase 2 Clinical
| M.Wt | 560.6375 | |
| Formula | C31H34F2N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 31 mg/mL |
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| 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]- |
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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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