AZD8931
AZD8931 Basic information
- Product Name:
- AZD8931
- Synonyms:
-
- 2-[4-[4-(3-chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]-N-methylacetamide
- AZD8931, >=96%
- AZD8931 (SAPITINIB);AZD 8931
- 4-(3-Chloro-2-fluoroanilino)-7-methoxy-6-[[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy]quina
- AZ08931 2-(4-(4-(3-chloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-N-methylacetamide
- 2-(4-(4-(3-chloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-N-methylacetamide
- Sapitinib(AZD8931)
- AZD8931
- CAS:
- 848942-61-0
- MF:
- C23H25ClFN5O3
- MW:
- 473.93
- Product Categories:
-
- Inhibitors
- Mol File:
- 848942-61-0.mol
AZD8931 Chemical Properties
- Boiling point:
- 632.8±55.0 °C(Predicted)
- Density
- 1.339
- storage temp.
- Store at -20°C
- solubility
- ≥23.7 mg/mL in DMSO; insoluble in H2O; ≥57.8 mg/mL in EtOH with gentle warming
- form
- solid
- pka
- 16.17±0.46(Predicted)
- color
- White to off-white
- InChIKey
- DFJSJLGUIXFDJP-UHFFFAOYSA-N
- SMILES
- N1(CC(NC)=O)CCC(OC2C(OC)=CC3C(C=2)=C(NC2=CC=CC(Cl)=C2F)N=CN=3)CC1
AZD8931 Usage And Synthesis
Uses
AZD8931 is a novel potent reversible small molecule epidermal growth factor receptor, ERBB2 (HER2) and ERBB3 inhibitor with an IC50 of 4, 3, 4 nM, respectively.
Definition
ChEBI: A member of the class of quinazolines that is 4-amino-7-methoxyquinazoline in which the amino group has been substituted by a 3-chloro-2-fluorophenyl group and in which position 6 of the quinoline ring has been substituted by a {1-[2-(methylamino)-2-oxoeth l]piperidin-4-yl}oxy group. Sapitinib is a dual tyrosine kinase inhibitor (TKI) of epithelial growth factor receptors (EGFR) HER2 and HER3.
Enzyme inhibitor
This signal transduction kinase inhibitor (FW = 473.94 g/mol; CAS 848942-61-0), also named 2-(4-[4-(3-chloro-2-fluorophenylamino)-7- methoxyquinazolin-6-yloxy]piperidin-1-yl)-N-methylacetamide, reversibly inhibits EGFR (IC50 = 4 nM), erbB2 (IC50 = 3 nM), and erbB3 (IC50 = 4 nM) phosphorylation in cells. In proliferation assays, AZD8931 is significantly more potent than gefitinib or lapatinib in specific squamous cell carcinoma of the head and neck and non-small cell lung carcinoma cell lines. In vivo, AZD8931 inhibits xenograft growth in a range of models, while significantly affecting EGFR, erbB2, and erbB3 phosphorylation and downstream signaling pathways, apoptosis, and proliferation. In EGF and HRG ligand-driven cell systems, AZD8931 is more potent than gefitinib or lapatinib. Metabolic disposition of AZD8931.
in vivo
AZD8931 (6.25-50 mg/kg, p.o.) significantly inhibits BT474c (breast), Calu-3 (NSCLC), LoVo (colorectal), FaDu (SCCHN), and PC-9 (NSCLC) tumor xenograft growth. AZD8931 is active in xenograft tumor models responsive to EGFR inhibition alone (LoVo and PC-9) or EGFR or erbB2 inhibition (BT474c, Calu-3, and FaDu). AZD8931 causes pharmacodynamic changes in proliferation and apoptosis markers in human tumor xenograft models[1]. AZD8931 (25 mg/kg, p.o.) significantly inhibits the growth of SUM149 and FC-IBC-02 cells in vivo in SCID mice[2]. AZD8931 displays favorable oral pharmacokinetics in rat and dog (low clearance and good bioavailability) and low human hepatocyte turnover (Clint < 4.5 μL/min/106 cells). In nude mouse after oral administration at 50 mg/kg, AZD8931 shows improved exposure, and at at 100 mg/kg oral dose once daily, it shows potent tumor growth inhibition activity in the LoVo mouse xenograft model[3].
target
ErbB2
IC 50
EGFR: 4 nM (IC50); ErbB2: 3 nM (IC50); HER3: 4 nM (IC50)
AZD8931Supplier
- Tel
- sales@boylechem.com
- Tel
- 21-57721279
- sales@shydchem.com.cn
- Tel
- 17702719238 18971495150;
- sales@sun-shinechem.com
- Tel
- 0531-88811783
- sales@trio-pharmatech.com
- Tel
- 0411-62910999 13889544652
- sales@meilune.com