Sapitinib (AZD8931)

製品コードS2192 バッチS219201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H25ClFN5O3
分子量 473.93 CAS No. 848942-61-0
Solubility (25°C)* 体外 DMSO 95 mg/mL (200.45 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.
in vitro AZD8931 shows different potency to NSCLC and SCCHN cell lines. AZD8931 has high sensitivity to PC-9 cells (EGFR activating mutation) with GI50 of 0.1 nM and low activity to NCI-1437 cells with GI50 above 10 μM. AZD8931 exhibits more potency against phospho-EGFR, phospho-erbB2 and phospho-erbB3 than either lapatinib or gefitinib in PE/CA-PJ41, PE/CA-PJ49, DOK and FaDu cells. [1]
in vivo AZD8931 reveals antitumor activity in BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts. AZD8931 could reduce p-Akt, Ki67 expression and p-ERK in BT474c xenografts following acute treatment. AZD8931 also causes induction of the M30 apoptosis marker. Furthermore, AZD8931 shows greater proapoptotic effect compared with gefitinib and lapatinib in LoVo xenografts. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Isolated kinase assays
The intracellular kinase domains of human EGFR and erbB2 are cloned and expressed in the baculovirus/Sf21 system. The inhibitory activity of AZD8931 is determined with ATP at Km concentrations (0.4 mM for erbB2 and 2 mM for EGFR) using the ELISA method.
細胞アッセイ 細胞株 Head and neck tumor cell lines (KYSE-30, OE21, PE/CA-PJ15, PE/CA-PJ34 (clone C12), PE/CA-PJ41 (clone D2), PE/CA-PJ49, DOK, Detroit562, RPMI2650, SCC-4, SCC-9, SCC-25, CAL 27, SW579, FaDu, Hs 840.T, KB, KYSE-450, and HEp-2, HN5) and NSCLC cell lines (PC-9,
濃度 0.001-10 μM
反応時間 96 hours
実験の流れ

To determine the antiproliferative activity against cell lines grown in vitro, AZD8931 is tested in a panel of NSCLC and SCCHN cell lines. Cells are incubated for 96 hours with AZD8931 (0.001-10 μM). Viable cell number is determined by 4 hours of incubation with MTS Colorimetric Assay reagent and absorbance measured at 490 nm on a spectrophotometer.
動物実験 動物モデル BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts in Swiss nude or severe combined immunodeficient (Charles River) mice.
投薬量 6.25-50 mg/kg
投与方法 Gavage

カスタマーフィードバック

Data from [J Immunol, 2014, 192(2), 722-31]

Data from [Data independently produced by , , J Pathol, 2016, 239(3):320-34.]

Data from [Data independently produced by , , Oncol Rep, 2016, 36(2):1000-6]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Irreversible HER2 inhibitors overcome resistance to the RSL3 ferroptosis inducer in non-HER2 amplified luminal breast cancer [ Cell Death Dis, 2023, 14(8):532] PubMed: 37596261
Colorectal Cancer Patient-Derived 2D and 3D Models Efficiently Recapitulate Inter- and Intratumoral Heterogeneity [ Adv Sci (Weinh), 2022, e2201539] PubMed: 35652270
Dual targeting of FGFR3 and ERBB3 enhances the efficacy of FGFR inhibitors in FGFR3 fusion-driven bladder cancer [ BMC Cancer, 2022, 22(1):478] PubMed: 35501832
Cooperative induction of receptor tyrosine kinases contributes to adaptive MAPK drug resistance in melanoma through the PI3K pathway [ Cancer Rep (Hoboken, 2022, e1736] PubMed: 36251678
STAT3 mediated upregulation of C-MET signaling acts as a compensatory survival mechanism upon EGFR family inhibition in chemoresistant breast cancer cells [ Cancer Lett, 2021, 519:328-342] PubMed: 34348188
Probing the signaling requirements for naive human pluripotency by high-throughput chemical screening [ Cell Rep, 2021, 35(11):109233] PubMed: 34133938
Heterotypic cell-cell communication regulates glandular stem cell multipotency [ Nature, 2020, 584(7822):608-613] PubMed: 32848220
Heterotypic cell-cell communication regulates glandular stem cell multipotency [ Nature, 2020, 584(7822):608-613] PubMed: 32848220
Therapeutic role of recurrent ESR1-CCDC170 gene fusions in breast cancer endocrine resistance [ Breast Cancer Res, 2020, 22(1):84] PubMed: 32771039
Efficient suppression of NRAS-driven melanoma by co-inhibition of ERK1/2 and ERK5 MAPK pathways. [ J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X] PubMed: 32376279

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人間や獣医の診断であるか治療的な使用のためにでない。

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