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Rociletinib hydrobromide (CO-1686 (hydrobromide))

رقم الكتالوجGC33061

Rociletinib hydrobromide (CO-1686 (hydrobromide)) (CO-1686 hydrobromide) هو مثبط كيناز يتم توصيله عن طريق الفم والذي يستهدف على وجه التحديد الأشكال الطافرة لـ EGFR بما في ذلك T790M ، وقيم Ki لـ EGFRL858R / T790M و EGFRWT هي 21.5 نانومتر و 303.3 نانومتر ، على التوالى.

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Rociletinib hydrobromide (CO-1686 (hydrobromide)) التركيب الكيميائي

Cas No.: 1446700-26-0

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
63٫00
متوفر
5mg
45٫00
متوفر
10mg
72٫00
متوفر
50mg
135٫00
متوفر
100mg
225٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition[1].

Rociletinib (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice[1].

[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.

مراجعات

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