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Datasheet of Entrectinib
Description: Entrectinib(NMS-E628、RXDX-101) is an orally available ALK inhibitor; exhibits good activity against NPM–ALK with an IC50 value of 55 nM. In vivo: study of NMSE628 showed complete tumor regression in both KARPAS-299 and SR-768 mouse xenograft models. When NMS-E628 was evaluated in Ba/F3–ALKL1196M and Ba/F3–ALKC1156Y cells that were identied in crizotinib resistant patients, it was able to inhibit them at lower dose than crizotinib, in both in vitro and in vivo conditions. NMS-E628 also showed ATP competitive inhibition of ROS1 with an IC50 value of 7 nM and induced complete tumor regression in Ba/F3-ROS1 mouse xenograft models for 10 days. It is currently being evaluated in phase I/II clinical trials.
Chemical Information Catalog
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Molecular Weight (MW)
Store at -20°C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Published on Sep 18, 2015