An EGFR and HER2 inhibitor
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Pyrotinib (maleate)

Item No. 42108

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-[(2R)-1-methyl-2-pyrrolidinyl]-2-propenamide, (2Z)-2-butenedioate
CAS Number
1397922-61-0
Synonyms
  • SHR-1258
Molecular Formula
C32H31ClN6O3 • 2C4H4O4
Formula Weight
815.2
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlDMSO: Sparingly Soluble: 1-10 mg/mlWater: Slightly Soluble: 0.1-1 mg/ml
SMILES
CCOC(C(NC(/C=C/[C@H]1CCCN1C)=O)=C2)=CC3=C2C(NC4=CC=C(C(Cl)=C4)OCC5=CC=CC=N5)=C(C#N)C=N3.OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O
InChi Code
InChI=1S/C32H31ClN6O3.2C4H4O4/c1-3-41-30-17-27-25(16-28(30)38-31(40)12-10-24-8-6-14-39(24)2)32(21(18-34)19-36-27)37-22-9-11-29(26(33)15-22)42-20-23-7-4-5-13-35-23;2*5-3(6)1-2-4(7)8/h4-5,7,9-13,15-17,19,24H,3,6,8,14,20H2,1-2H3,(H,36,37)(H,38,40);2*1-2H,(H,5,6)(H,7,8)/b12-10+;2*2-1-/t24-;;/m1../s1
InChi Key
KLHFGQSCVQPTIN-XUZAKNADSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $153

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    10 mg

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    25 mg

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    Product Description

    Pyrotinib is an inhibitor of EGFR and HER2 (IC50s = 13 and 38 nM, respectively).1 It selectively inhibits the proliferation of HER2-positive BT474 breast and SKOV3 ovarian cancer cells (IC50s = 5.1 and 43 nM, respectively) over HER2-negative MDA-MB-231 breast cancer cells (IC50 = 3,500 nM). In vivo, pyrotinib (10 mg/kg per day) decreases tumor growth without affecting body weight in BT474 and SKOV3 mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, X., Yang, C., Wan, H., et al. Discovery and development of pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer. Eur. J. Pharm. Sci. 110, 51-61 (2017).