Sapitinib (AZD8931)

Catalog No.S2192

Sapitinib (AZD8931) Chemical Structure

Molecular Weight(MW): 473.93

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 than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.

Size Price Stock Quantity  
In DMSO USD 320 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 24 Publications

Purity & Quality Control

Choose Selective HER2 Inhibitors

Biological Activity

Description 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 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. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7 cells NH;qcJJHfW6ldHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKGincnXneYxqdi2|dHnteYxifGWmIFjFVlIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1ETjdiY3XscJMtKEmFNUC9N{BvVQ>? M4\v[lI1QTByN{Sx
human KB cells NEXWelJHfW6ldHnvckBie3OjeR?= M3;GcWlvcGmkaYTpc44hd2ZiRVfGMZN1cW23bHH0[YQhTUeIUjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iS1KgZ4VtdHNuIFnDOVA:PCCwTR?= NYH0[2d3OjR7MEC3OFE>
human MCF7 cells NWXRWWRTTnWwY4Tpc44h[XO|YYm= M3zsRWlvcGmkaYTpc44hd2ZiaHXy[Yd2dGmwLYP0bY12dGG2ZXSgTGVTOyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hVUOINzDj[YxteyxiSVO1NF01KG6P NIeyVG8zPDlyMEe0NS=>
human MCF-7 cl.24 cells MYTGeY5kfGmxbjDhd5NigQ>? M2TDdFQhcA>? NH;LXYdKdmirYnn0bY9vKG:oIH\1cIwudGWwZ4ToJGhGWjJicHjvd5Bpd3K7bHH0bY9vKHS{YX7z[oVkfGWmIHnuJIlvKGi3bXHuJG1ETi15IHPsMlI1KGOnbHzzJIFnfGW{IESgbJJ{KGK7IHzhd4VzKHOlYX7ubY5oKG[udX;y[ZNk\W6lZTDtbYNzd3CuYYTlJIN6fG:vZYTyfUwhUUN3ME22NEBvVQ>? NYq5U3BCOjR7MEC3OFE>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
pEGFR / EGFR / pAKT / AKT / pERK / ERK ; 

PubMed: 27102572     


Western blot analysis confirm suppression of the biomarker p-EGFR upon treatment with EGFR TKIs in U-CH1 and UM-Chor1. Cells were serum-starved overnight before they were treated with a range of concentrations of the EGFR inhibitors for 4 h and then EGF-spiked (50 ng/ml) for 15 min. Endogenous controls (non-serum-starved, non-EGF-spiked), untreated controls (serum-starved, non-EGF-spiked) and vehicle controls (serum‐starved, treated with 2.5% DMSO, EGF-spiked) were included.

HER3 / p-HER3 / HER2 / p-HER2 / p-PRAS40 / p-S6 / p-4EBP1 / p-FOXO / PARP / cleaved PARP; 

PubMed: 26095475     


(A) BT474c or HCC1954 cells were treated for 24 h with increasing concentrations of AZD5363 ±0.3 μM or 1 μM AZD8931, respectively. Protein lysates were analysed by immunoblot with the indicated antibodies. Blots are representative of blots from 2–3 separate experiments.

27102572 26095475
Growth inhibition assay
Cell viability; 

PubMed: 28638122     


Growth control graphs showing effect of selected HER-family TKIs in doubling concentrations on growth of breast cancer cell lines. (a) EGFR reversible inhibitor erlotinib. (b) Dual EGFR/HER2 reversible inhibitor lapatinib. (c) Pan-HER reversible inhibitor sapitinib. (d) Pan-HER irreversible inhibitor canertinib. (e) Pan-HER irreversible inhibitor afatinib. Sulforhodamine B colorimetric assay was used to determine the effect of treatment of breast cancer cell lines with doubling dilutions of HER-family inhibiting TKIs. The irreversible pan-inhibitors (e.g. afatinib, canertinib, neratinib) were consistently more effective than the reversible dual and pan inhibitors (e.g. lapatinib, sapitinib), which were in turn more effective than the reversible EGFR inhibitors (e.g. erlotinib, gefitinib). Each point is a representative of the mean ± SD of triplicate samples.

28638122
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]

Protocol

Kinase Assay:

[1]
- Collapse

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:

[1]
- Collapse
  • Cell lines: 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,
  • Concentrations: 0.001-10 μM
  • Incubation Time: 96 hours
  • Method:

    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)
Animal Research:

[1]
- Collapse
  • Animal Models: BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts in Swiss nude or severe combined immunodeficient (Charles River) mice.
  • Formulation: Suspended in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween 80) in deionized water
  • Dosages: 6.25-50 mg/kg
  • Administration: Gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (84.4 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing. 		5 mg/mL

* 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.

Chemical Information

Molecular Weight 473.93
Formula

C23H25ClFN5O3
CAS No. 848942-61-0
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01596530 Terminated Drug: Drug-AZD8931|Drug: Drug-Placebo Breast Neoplasm AstraZeneca June 2012 Phase 1
NCT01579578 Terminated Drug: AZD8931|Drug: Placebo|Drug: Paclitaxel Metastatic Gastric or Gastro-oesophageal Junction Cancer AstraZeneca April 2012 Phase 2
NCT01330758 Completed Drug: AZD8931 Healthy AstraZeneca April 2011 Phase 1
NCT01284595 Completed Drug: [14C] AZD8931 Healthy AstraZeneca March 2011 Phase 1
NCT01151215 Terminated Drug: AZD8931|Drug: anastrozole|Drug: Placebo Neoplasms|Breast Neoplasms|Breast Cancer AstraZeneca June 2010 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
selleck catalog

HER2 Signaling Pathway Map

HER2 Inhibitors with Unique Features

Related HER2 Products

  • Erlotinib New

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • R428 (BGB324，Bemcentinib) New

    R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

  • Pexidartinib (PLX3397) New

    Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.

  • Lapatinib (GW-572016) Ditosylate

    Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

  • AC480 (BMS-599626)

    AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.

  • CP-724714

    CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.

  • Neratinib (HKI-272)

    Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.

  • Mubritinib (TAK 165)

    Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. Phase 1.

  • Tyrphostin AG 879

    Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.

  • Gefitinib (ZD1839)

    Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

    Features:A potent EGFR tyrosine kinase inhibitor.

Tags: buy Sapitinib (AZD8931) | Sapitinib (AZD8931) supplier | purchase Sapitinib (AZD8931) | Sapitinib (AZD8931) cost | Sapitinib (AZD8931) manufacturer | order Sapitinib (AZD8931) | Sapitinib (AZD8931) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID