ChemicalBook > CAS DataBase List > AZD8931

AZD8931

Product Name
AZD8931
CAS No.
848942-61-0
Chemical Name
AZD8931
Synonyms
CS-368;AZD8931;Sapitinib;AZD8931, >=96%;AZD8931 USP/EP/BP;Sapitinib(AZD8931);AZD8931 (Sapitinib);Sapitinib, 10 mM in DMSO;AZD-8931;AZD8931;AZD 8931;AZD8931 (SAPITINIB);AZD 8931
CBNumber
CB22518215
Molecular Formula
C23H25ClFN5O3
Formula Weight
473.93
MOL File
848942-61-0.mol
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AZD8931 Property

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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H302Harmful if swallowed

H360May damage fertility or the unborn child

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P314Get medical advice/attention if you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
24196
Product name
AZD 8931
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
24196
Product name
AZD 8931
Purity
≥98%
Packaging
5mg
Price
$140
Updated
2024/03/01
Cayman Chemical
Product number
24196
Product name
AZD 8931
Purity
≥98%
Packaging
10mg
Price
$235
Updated
2024/03/01
Cayman Chemical
Product number
24196
Product name
AZD 8931
Purity
≥98%
Packaging
25mg
Price
$533
Updated
2024/03/01
ApexBio Technology
Product number
A8375
Product name
AZD8931(Sapitinib)
Packaging
50mg
Price
$599
Updated
2021/12/16
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AZD8931 Chemical Properties,Usage,Production

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)

AZD8931 Preparation Products And Raw materials

Raw materials

Preparation Products

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AZD8931 Suppliers

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View Lastest Price from AZD8931 manufacturers

Hebei Yanxi Chemical Co., Ltd.
Product
AZD8931 848942-61-0
Price
US $0.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
20tons
Release date
2023-10-09
Zhuozhou Wenxi import and Export Co., Ltd
Product
Sapitinib 848942-61-0
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Sapitinib 848942-61-0
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-09

848942-61-0, AZD8931Related Search:

Lapatinib MK-2206 2HCl Erlotinib hydrochloride Ibrutinib Afatinib Olaparib

  • 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
  • 4-(3-Chloro-2-fluoroanilino)-7-methoxy-6-[[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy]quinazoline
  • Sapitinib
  • AZD8931 (Sapitinib)
  • CS-368
  • AZD-8931;AZD8931;AZD 8931
  • 2-[4-({4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl}oxy)-1-piperidinyl]-N-methylacetamide
  • 1-Piperidineacetamide, 4-[[4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-methyl-
  • AZD8931 USP/EP/BP
  • 2-[4-({4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinaz...
  • Sapitinib, 10 mM in DMSO
  • 848942-61-0
  • C23H25ClFN5O3
  • Inhibitors