An inhibitor of BRK/PTK6
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Tilfrinib

Item No. 25647

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(9H-pyrido[2,3-b]indol-4-ylamino)-phenol
CAS Number
1600515-49-8
Molecular Formula
C17H13N3O
Formula Weight
275.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 23 mg/mlEthanol: 13 mg/ml
SMILES
OC1=CC=CC(NC2=CC=NC3=C2C4=C(C=CC=C4)N3)=C1
InChi Code
InChI=1S/C17H13N3O/c21-12-5-3-4-11(10-12)19-15-8-9-18-17-16(15)13-6-1-2-7-14(13)20-17/h1-10,21H,(H2,18,19,20)
InChi Key
RXPZOSHFGJWSLQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $50

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    5 mg

    $134

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    10 mg

    $242

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    25 mg

    $543

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    Product Description

    Tilfrinib is an inhibitor of breast tumor kinase/protein tyrosine kinase 6 (BRK/PTK6; IC50 = 3.15 nM).1,2 It is selective for BRK/PTK6 over HER2 (IC50 = 1,300 nM).2 Tilfrinib inhibits the growth of MCF-7, HS-578/T, and BT-549 breast cancer cells in vitro (GI50s = 0.99, 1.02, and 1.58 μM, respectively).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mahmoud, K.A., Krug, M., Wersig, T., et al. Discovery of 4-anilino α-carbolines as novel Brk inhibitors. Bioorg. Med. Chem. Lett. 24(8), 1948-1951 (2014).

    2. Mahmoud, K.A., Wersig, T., Slynko, I., et al. Novel inhibitors of breast cancer relevant kinases Brk and HER2. Med. Chem. Commun. 5, 659-664 (2014).