AZD-8931 - CAS 848942-61-0
Catalog number: B0084-286313
Category: Inhibitor
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Molecular Formula:
C23H25ClFN5O3
Molecular Weight:
473.933
COA:
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Targets:
EGFR
Description:
Sapitinib, also known as AZD-8931, is an erbB receptor tyrosine kinase inhibitor with potential antineoplastic activity. AZD8931 binds to and inhibits erbB tyrosine receptor kinases, which may result in the inhibition of cellular proliferation and angiogenesis in tumors expressing erbB.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-286313 100 mg $198 In stock
B0084-286313 500 mg $798 In stock
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Purity:
0.98
Appearance:
Solid powder
Synonyms:
AZD8931; AZD 8931; Momelotinib; Sapitinib.
MSDS:
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InChIKey:
DFJSJLGUIXFDJP-UHFFFAOYSA-N
InChI:
InChI=1S/C23H25ClFN5O3/c1-26-21(31)12-30-8-6-14(7-9-30)33-20-10-15-18(11-19(20)32-2)27-13-28-23(15)29-17-5-3-4-16(24)22(17)25/h3-5,10-11,13-14H,6-9,12H2,1-2H3,(H,26,31)(H,27,28,29)
Canonical SMILES:
CNC(=O)CN1CCC(CC1)OC2=C(C=C3C(=C2)C(=NC=N3)NC4=C(C(=CC=C4)Cl)F)OC
1.The first radiosynthesis of [(11)C]AZD8931 as a new potential PET agent for imaging of EGFR, HER2 and HER3 signaling.
Wang M;Gao M;Zheng QH Bioorg Med Chem Lett. 2014 Sep 15;24(18):4455-4459. doi: 10.1016/j.bmcl.2014.07.092. Epub 2014 Aug 8.
The reference standard AZD8931{2-(4-((4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)-N-methylacetamide} (11a) was synthesized from methyl 4,5-dimethoxy-2-nitrobenzoate or ethyl 4,5-dimethoxy-2-nitrobenzoate and 2-chloro-N-methylacetamide in 11 steps with 2-5% overall chemical yield. The precursor N-desmethyl-AZD8931{2-(4-((4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)acetamide} (11b) was synthesized from methyl 4,5-dimethoxy-2-nitrobenzoate or ethyl 4,5-dimethoxy-2-nitrobenzoate and 2-bromoacetamide in 11 steps with 2-4% overall chemical yield. The target tracer [(11)C]AZD8931 {2-(4-((4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)-N-[(11)C]methylacetamide} ([(11)C]11a) was prepared from N-desmethyl-AZD8931 (11b) with [(11)C]CH3OTf under basic condition (NaH) through N-[(11)C]methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 40-50% radiochemical yield based on [(11)C]CO2 and decay corrected to end of bombardment (EOB) with 370-1110GBq/μmol specific activity at EOB.
2.Impact of the putative cancer stem cell markers and growth factor receptor expression on the sensitivity of ovarian cancer cells to treatment with various forms of small molecule tyrosine kinase inhibitors and cytotoxic drugs.
Puvanenthiran S;Essapen S;Seddon AM;Modjtahedi H Int J Oncol. 2016 Nov;49(5):1825-1838. doi: 10.3892/ijo.2016.3678. Epub 2016 Sep 5.
Increased expression and activation of human epidermal growth factor receptor (EGFR) and HER-2 have been reported in numerous cancers. The aim of this study was to determine the sensitivity of a large panel of human ovarian cancer cell lines (OCCLs) to treatment with various forms of small molecule tyrosine kinase inhibitors (TKIs) and cytotoxic drugs. The aim was to see if there was any association between the protein expression of various biomarkers including three putative ovarian cancer stem cell (CSC) markers (CD24, CD44, CD117/c-Kit), P-glycoprotein (P-gp), and HER family members and response to treatment with these agents. The sensitivity of 10 ovarian tumour cell lines to the treatment with various forms of HER TKIs (gefitinib, erlotinib, lapatinib, sapitinib, afatinib, canertinib, neratinib), as well as other TKIs (dasatinib, imatinib, NVP-AEW541, crizotinib) and cytotoxic agents (paclitaxel, cisplatin and doxorubicin), as single agents or in combination, was determined by SRB assay. The effect on these agents on the cell cycle distribution, and downstream signaling molecules and tumour migration were determined using flow cytometry, western blotting, and the IncuCyte Clear View cell migration assay respectively.
3.EGFR inhibitors identified as a potential treatment for chordoma in a focused compound screen.
Scheipl S;Barnard M;Cottone L;Jorgensen M;Drewry DH;Zuercher WJ;Turlais F;Ye H;Leite AP;Smith JA;Leithner A;Möller P;Brüderlein S;Guppy N;Amary F;Tirabosco R;Strauss SJ;Pillay N;Flanagan AM J Pathol. 2016 Jul;239(3):320-34. doi: 10.1002/path.4729. Epub 2016 May 31.
Chordoma is a rare malignant bone tumour with a poor prognosis and limited therapeutic options. We undertook a focused compound screen (FCS) against 1097 compounds on three well-characterized chordoma cell lines; 154 compounds were selected from the single concentration screen (1 µm), based on their growth-inhibitory effect. Their half-maximal effective concentration (EC50 ) values were determined in chordoma cells and normal fibroblasts. Twenty-seven of these compounds displayed chordoma selective cell kill and 21/27 (78%) were found to be EGFR/ERBB family inhibitors. EGFR inhibitors in clinical development were then studied on an extended cell line panel of seven chordoma cell lines, four of which were sensitive to EGFR inhibition. Sapitinib (AstraZeneca) emerged as the lead compound, followed by gefitinib (AstraZeneca) and erlotinib (Roche/Genentech). The compounds were shown to induce apoptosis in the sensitive cell lines and suppressed phospho-EGFR and its downstream pathways in a dose-dependent manner. Analysis of substituent patterns suggested that EGFR-inhibitors with small aniline substituents in the 4-position of the quinazoline ring were more effective than inhibitors with large substituents in that position.
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CAS 848942-61-0 AZD-8931

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