Rociletinib - CAS 1374640-70-6
Catalog number: B0084-462150
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Rociletinib is a third-generation irreversible kinase inhibitor of epidermal growth factor receptor (EGFR). Rociletinib was shown to inhibit the proliferation of non-small cell lung cancer (NSCLC) cells expressing mutant EGFR. It also exhibits anti-tumor activity in NSCLC EGFR mutant xenograft models.
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Catalog Number Size Price Stock Quantity
B0084-462150 100 mg $198 In stock
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Brife Description:
third-generation EGFR inhibitor
Off-White Solid
CO-1686; CO1686; CO 1686; AVL-301; AVL 301; AVL301; CNX-419; CNX 419; CNX419; N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
Melting Point:
202 - 205°C (dec.)
Canonical SMILES:
1.Increased Expression of IRE1α Associates with the Resistant Mechanism of Osimertinib (AZD9291)-resistant non-small Cell Lung Cancer HCC827/OSIR Cells.
Tang ZH;Su MX;Guo X;Jiang XM;Jia L;Chen X;Lu JJ Anticancer Agents Med Chem. 2018;18(4):550-555. doi: 10.2174/1871520617666170719155517.
BACKGROUND: ;Osimertinib (OSI), also known as AZD9291, is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that has been approved for the treatment of non-small cell lung cancer (NSCLC) patients.;OBJECTIVE: ;Establishment of the OSI-resistant HCC827/OSIR cell line and study of its resistant mechanism.;METHOD: ;The anti-proliferative effect was studied through MTT and colony formation assays. The protein expression was detected by Western blot assay. The gene was silenced by small interfering RNA. The cellular morphology was observed by using an optical microscope. The viable cell numbers were counted by trypan blue staining assay.;RESULTS: ;The OSI-resistant HCC827/OSIR cells were established on HCC827 cells with naive EGFR-sensitive mutation, and the resistant effects of HCC827/OSIR cells were confirmed through MTT and colony formation assays. The IC50s of HCC827/OSIR cells to other EGFR TKIs, such as gefitinib, erlotinib, afatinib, and rociletinib was higher than that of the HCC827 cells. The anti-proliferative effects of paclitaxel, pemetrexed, doxorubicin, and fluorouracil in HCC827 and HCC827/OSIR cells were similar. The expression of inositolrequiring enzyme 1α (IRE1α) was increased after the cells developed resistance to OSI.
2.EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or Third-Generation TKIs.
Kobayashi Y;Togashi Y;Yatabe Y;Mizuuchi H;Jangchul P;Kondo C;Shimoji M;Sato K;Suda K;Tomizawa K;Takemoto T;Hida T;Nishio K;Mitsudomi T Clin Cancer Res. 2015 Dec 1;21(23):5305-13. doi: 10.1158/1078-0432.CCR-15-1046. Epub 2015 Jul 23.
PURPOSE: ;Lung cancers harboring common EGFR mutations respond to EGFR tyrosine kinase inhibitors (TKI), whereas exon 20 insertions (Ins20) are resistant to them. However, little is known about mutations in exon 18.;EXPERIMENTAL DESIGN: ;Mutational status of lung cancers between 2001 and 2015 was reviewed. Three representative mutations in exon 18, G719A, E709K, and exon 18 deletion (Del18: delE709_T710insD) were retrovirally introduced into Ba/F3 and NIH/3T3 cells. The 90% inhibitory concentrations (IC90s) of first-generation (1G; gefitinib and erlotinib), second-generation (2G; afatinib, dacomitinib, and neratinib), and third-generation TKIs (3G; AZD9291 and CO1686) were determined.;RESULTS: ;Among 1,402 EGFR mutations, Del19, L858R, and Ins20 were detected in 40%, 47%, and 4%, respectively. Exon 18 mutations, including G719X, E709X, and Del18, were present in 3.2%. Transfected Ba/F3 cells grew in the absence of IL3, and NIH/3T3 cells formed foci with marked pile-up, indicating their oncogenic abilities. IC90s of 1G and 3G TKIs in G719A, E709K, and Del18 were much higher than those in Del19 (by >11-50-fold), whereas IC90s of afatinib were only 3- to 7-fold greater than those for Del19.
3.AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients.
Xu X;Mao L;Xu W;Tang W;Zhang X;Xi B;Xu R;Fang X;Liu J;Fang C;Zhao L;Wang X;Jiang J;Hu P;Zhao H;Zhang L Mol Cancer Ther. 2016 Nov;15(11):2586-2597. Epub 2016 Aug 29.
AC0010 is a pyrrolopyrimidine-based irreversible EGFR inhibitor, structurally distinct from previously reported pyrimidine-based irreversible EGFR inhibitors, such as osimertinib and rociletinib. AC0010 selectively inhibits EGFR-active and T790M mutations with up to 298-fold increase in potency compared with wild-type EGFR. In a xenograft model, oral administration of AC0010 at a daily dose of 500 mg/kg resulted in complete remission of tumors with EGFR-active and T790M mutations for over 143 days with no weight loss. Three major metabolites of AC0010 were tested and showed no wild-type EGFR inhibition or off-target effects, such as inhibition of IGF-1R. AC0010 is safe in non-small cell lung cancer (NSCLC) patients at a dose range between 50 and 550 mg once per day, and no hyperglycemia or other severe adverse effects were detected, such as grade 3 QT prolongation. The objective responses were observed in NSCLC patients with EGFR T790M mutation. Mol Cancer Ther; 15(11); 2586-97.;©2016 AACR.
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CAS 1374640-70-6 Rociletinib

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