An inhibitor of mutant EGFR
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HM61713

Item No. 19481

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]thieno[3,2-d]pyrimidin-4-yl]oxy]phenyl]-2-propenamide
CAS Number
1353550-13-6
Synonyms
  • BI-1482694
  • Olmutinib
Molecular Formula
C26H26N6O2S
Formula Weight
486.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 44 mg/mL
SMILES
CN1CCN(C2=CC=C(NC3=NC(OC4=CC=CC(NC(C=C)=O)=C4)=C(SC=C5)C5=N3)C=C2)CC1
InChi Code
InChI=1S/C26H26N6O2S/c1-3-23(33)27-19-5-4-6-21(17-19)34-25-24-22(11-16-35-24)29-26(30-25)28-18-7-9-20(10-8-18)32-14-12-31(2)13-15-32/h3-11,16-17H,1,12-15H2,2H3,(H,27,33)(H,28,29,30)
InChi Key
FDMQDKQUTRLUBU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    25 mg

    $587

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    Product Description

    HM61713 is an inhibitor of mutant EGFR (IC50 = 0.01 µM for EGFRT790M/L858R).1 It is selective for EGFRT790M/L858R over PI3Kα (IC50 = >10 µM). HM61713 is cytotoxic to A549, H1975, and H460 lung and MCF-7 breast cancer cells (IC50s = 4.29, 0.52, 5.29, and 26.9 µM, respectively). It reduces tumor growth in an ETS1-overexpressing doxorubicin-resistant K562 leukemia mouse xenograft model when administered at a dose of 30 mg/kg in combination with doxorubicin.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hu, X., Tang, S., Yang, F., et al. Design, synthesis, and antitumor activity of olmutinib derivatives containing acrylamide moiety. Molecules 26(10), 3041 (2021).

    2. Zhong, J., Zhang, J., Yu, X., et al. Olmutinib reverses doxorubicin resistance in ETS1-overexpressing leukemia cells. Med. Sci. Monit. 26, e924922 (2020).