A dual inhibitor of EGFR and HER2
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TAK-285

Item No. 29157

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[4-[[3-chloro-4-[3-(trifluoromethyl)phenoxy]phenyl]amino]-5H-pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methyl-butanamide
CAS Number
871026-44-7
Molecular Formula
C26H25ClF3N5O3
Formula Weight
548.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: 10 mg/ml
λmax
215, 306 nm
SMILES
CC(C)(O)CC(NCCN1C=CC2=NC=NC(NC3=CC=C(OC4=CC=CC(C(F)(F)F)=C4)C(Cl)=C3)=C21)=O
InChi Code
InChI=1S/C26H25ClF3N5O3/c1-25(2,37)14-22(36)31-9-11-35-10-8-20-23(35)24(33-15-32-20)34-17-6-7-21(19(27)13-17)38-18-5-3-4-16(12-18)26(28,29)30/h3-8,10,12-13,15,37H,9,11,14H2,1-2H3,(H,31,36)(H,32,33,34)
InChi Key
ZYQXEVJIFYIBHZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    TAK-285 is a dual inhibitor of EGFR and HER2 (IC50s = 23 and 17 nM, respectively).1 It is selective for EGFR and HER2 over a panel of 36 kinases (IC50s = 250->10,000 nM). TAK-285 inhibits the proliferation of BT474 breast cancer cells (GI50 = 17 nM) as well as induces tumor regression in a 4-1st gastric adenocarcinoma rat xenograft model when administered at doses of 25 and 50 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ishikawa, T., Seto, M., Banno, H., et al. Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. J. Med. Chem. 54(23), 8030-8050 (2011).