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Sapitinib

Catalog No. T6092 CAS 848942-61-0

Synonyms: AZD-8931

Sapitinib (AZD-8931) , a reversible, ATP competitive inhibitor of EGFR(IC50=4 nM), ErbB2(IC50=3 nM) and ErbB3(IC50=4 nM), is more effective over Gefitinib or Lapatinib against NSCLC cell, 100-fold more specific for the ErbB family over MNK1 and Flt.

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Sapitinib, CAS 848942-61-0

Pack Size	Availability	Price/USD
2 mg	In stock	$ 32.00
5 mg	In stock	$ 52.00
10 mg	In stock	$ 79.00
25 mg	In stock	$ 113.00
50 mg	In stock	$ 169.00
100 mg	In stock	$ 252.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 99.83%

Purity: 98.35%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Sapitinib (AZD-8931) , a reversible, ATP competitive inhibitor of EGFR(IC50=4 nM), ErbB2(IC50=3 nM) and ErbB3(IC50=4 nM), is more effective over Gefitinib or Lapatinib against NSCLC cell, 100-fold more specific for the ErbB family over MNK1 and Flt.
Targets&IC50	EGFR:4 nM, ErbB2:3 nM, ERB3:4 nM
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]
Kinase Assay	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.
Cell Research	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. (Only for Reference)

Synonyms	AZD-8931
Molecular Weight	473.93
Formula	C23H25ClFN5O3
CAS No.	848942-61-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 38 mg/mL (80.2 mM)

References and Literature

1. Hickinson DM, et al. Clin Cancer Res, 2010, 16(4), 1159-1169.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Bioactive Compounds Library Max Anti-Breast Cancer Compound Library

Related Products

Related compounds with same targets

Naquotinib (S)-Afatinib 4-Hydroxycinnamamide EGFR/CDK2-IN-3 Osimertinib mesylate Dacomitinib EGFR-IN-82 (E/Z)-CP-724714

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Keywords

Sapitinib 848942-61-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR inhibit Inhibitor HER1 ErbB-1 AZD8931 Epidermal growth factor receptor AZD 8931 AZD-8931 inhibitor

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