Entrectinib (NMS-E628, RXDX-101) | ROS1/TRK/ALK inhibitor

Chemical Structure : Entrectinib

CAS No.: 1108743-60-7

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

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
25 mg	$148	In stock
50 mg	$238	In stock
100 mg	$388	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	560.6375
Formula	C31H34F2N6O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
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]-

References

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.

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

Biological Activity

Physicochemical Properties

References

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