An ALK5 inhibitor
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BIBF 0775

Item No. 37777

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3Z)-N-ethyl-2,3-dihydro-N-methyl-2-oxo-3-[phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indole-6-carboxamide
CAS Number
334951-90-5
Molecular Formula
C31H34N4O2
Formula Weight
494.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 5 mg/mlEthanol: 2 mg/ml
λmax
283, 387 nm
SMILES
O=C1NC2=CC(C(N(C)CC)=O)=CC=C2/C1=C(C3=CC=CC=C3)/NC4=CC=C(C=C4)CN5CCCCC5
InChi Code
InChI=1S/C31H34N4O2/c1-3-34(2)31(37)24-14-17-26-27(20-24)33-30(36)28(26)29(23-10-6-4-7-11-23)32-25-15-12-22(13-16-25)21-35-18-8-5-9-19-35/h4,6-7,10-17,20,32H,3,5,8-9,18-19,21H2,1-2H3,(H,33,36)/b29-28-
InChi Key
MUSRTIADFPCYTQ-ZIADKAODSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $183

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    10 mg

    $284

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    25 mg

    $556

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    Product Description

    BIBF 0775 is an inhibitor of TGF-β receptor type 1 (ALK5; IC50 = 34 nM).1 It is selective for ALK5 over VEGFR2 and PDGFRα (IC50s = 1,447 and 890 nM, respectively), as well as a panel of 30 other kinases at 1 µM.1,2 BIBF 0775 inhibits the phosphorylation of SMAD2 and SMAD3 in HaCaT cells (EC50 = 105 nM) and is not cytotoxic to HaCaT cells (IC50 = >1,000 nM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Roth, G.J., Heckel, A., Brandl, T., et al. Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factor β receptor I (TGFβRI). J. Med. Chem. 53(20), 7287-7295 (2010).

    2. Roth, G.J., Heckel, A., Colbatzky, F., et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). J. Med. Chem. 52(14), 4466-4480 (2009).