[CAS NO. 848942-61-0] Sapitinib (AZD8931)

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PRODUCTS SPECIFICATIONS [848942-61-0]

Catalog

SLK-S2192

Brand

Selleck

CAS

848942-61-0

DESCRIPTION [848942-61-0]

Overview

MDL	MFCD18385011
Molecular Weight	473.93
Molecular Formula	C23H25ClFN5O3
SMILES	N(C=1C2=C(C=C(OC)C(OC3CCN(CC(NC)=O)CC3)=C2)N=CN1)C4=C(F)C(Cl)=CC=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of , and with 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.

Targets

ErbB2 ^[1] (Cell-free assay)	EGFR ^[1] (Cell-free assay)	ErbB3 ^[1] (Cell-free assay)
3 nM	4 nM	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.

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.

References

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

Synonyms

1-Piperidineacetamide, 4-[[4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-methyl-

4-[[4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-methyl-1-piperidineacetamide

4-(3-Chloro-2-fluoroanilino)-7-methoxy-6-[[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy]quinazoline

AZD 8931

Sapitinib

Sapatinib

2-[4-[4-(3-Chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]-N-methylacetamide