A reversible inhibitor of ErbB1/EGFR, ErbB2/HER2, and ErbB3/HER3
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AZD 8931

Item No. 24196

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-methyl-1-piperidineacetamide
CAS Number
848942-61-0
Synonyms
  • Sapitinib
Molecular Formula
C23H25ClFN5O3
Formula Weight
473.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMF:PBS (pH 7) (1:10): 0.09 mg/mlDMSO: 25 mg/ml
λmax
250, 330 nm
SMILES
O=C(NC)CN1CCC(OC2=CC(C(NC3=CC=CC(Cl)=C3F)=NC=N4)=C4C=C2OC)CC1
InChi Code
InChI=1S/C23H25ClFN5O3/c1-26-21(31)12-30-8-6-14(7-9-30)33-20-10-15-18(11-19(20)32-2)27-13-28-23(15)29-17-5-3-4-16(24)22(17)25/h3-5,10-11,13-14H,6-9,12H2,1-2H3,(H,26,31)(H,27,28,29)
InChi Key
DFJSJLGUIXFDJP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $49

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    5 mg

    $154

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    10 mg

    $259

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    25 mg

    $587

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    Product Description

    AZD 8931 is a reversible inhibitor of the receptor tyrosine kinases ErbB1/EGFR, ErbB2/HER2, and ErbB3/HER3 (IC50s = 4, 3, and 4 nM, respectively, for autophosphorylation).1 In vitro, AZD 8931 (0.01, 0.1, and 1 µM) suppresses cell growth and induces apoptosis in SUM149 and FC-IBC-02 human breast cancer cell lines.2 In vivo, AZD 8931 (6.25-50 mg/kg) inhibits tumor growth in BT474c, Calu-3, LoVo, FaDu, and PC-9 mouse xenograft models.1 When administered in combination with paclitaxel (Item No. 10461), AZD 8931 inhibits inflammatory breast cancer tumor growth in a mouse xenograft model when administered at a dose of 25 mg/kg per day.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hickinson, D.M., Klinowska, T., Speake, G., et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: A unique agent for simultaneous ERBB receptor blockade in cancer. Clin. Cancer Res. 16(4), 1159-1169 (2010).

    2. Mu, Z., Klinowska, T., Dong, X., et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor (EGFR), HER2, and HER3: Preclinical activity in HER2 non-amplified inflammatory breast cancer models. J. Exp. Clin. Cancer Res. 33:47, (2014).