Sapitinib (AZD8931)

製品コードS2192 バッチS219203

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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
30%PEG400 0.5%Tween80 5%propylene glycol

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (10.55mM) Taking the 1 mL working solution as an example, add 300 μL of 16.67 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.
in vitro

Sapitinib (AZD8931) shows different potency to NSCLC and SCCHN cell lines, with 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. It exhibits more potency against phospho-EGFR, phospho-erbB2 and phospho-erbB3 in PE/CA-PJ41, PE/CA-PJ49, DOK and FaDu cells. [1]
in vivo

Sapitinib (AZD8931) reveals antitumor activity in BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts. It could reduce p-Akt, Ki67 expression and p-ERK in BT474c xenografts following acute treatment. This compound also causes induction of the M30 apoptosis marker. Furthermore, it shows greater proapoptotic effect 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
Sapitinib (AZD8931) is evaluated using the intracellular kinase domains of human EGFR and erbB2, which are cloned and expressed in the baculovirus/Sf21 system. Its inhibitory activity 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 of Sapitinib (AZD8931) against cell lines grown in vitro, it is tested in a panel of NSCLC and SCCHN cell lines. Cells are incubated for 96 hours with this compound (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

参考

  • https://pubmed.ncbi.nlm.nih.gov/20145185/

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：

PI3K-dependent GAB1/Erk phosphorylation renders head and neck squamous cell carcinoma sensitive to PI3Kα inhibitors [ Cell Death Dis, 2025, 16(1):457] PubMed: 40533463
LIFR-Mediated ERBB2 Signaling Is Essential for Successful Embryo Implantation in Mice [ Biomolecules, 2025, 15(5)698] PubMed: 40427591
Targeting ERBB3 and AKT to overcome adaptive resistance in EML4-ALK-driven non-small cell lung cancer [ Cell Death Dis, 2024, 15(12):912] PubMed: 39695132
Identification of kinase modulators as host-directed therapeutics against intracellular methicillin-resistant Staphylococcus aureus [ Front Cell Infect Microbiol, 2024, 14:1367938] PubMed: 38590439
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
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
Simultaneous Inhibition of ErbB3 and Calmodulin-Mediated Signaling Effectively Inhibits Malignant Peripheral Nerve Sheath Tumor Proliferation and Survival [ Medical University of South Carolina, 2023, ] PubMed: None
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

長期の保管のために-20°Cの下で製品を保ってください。

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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