An orally bioavailable tyrosine kinase inhibitor
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Rebastinib

Item No. 21465

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[[[[3-(1,1-dimethylethyl)-1-(6-quinolinyl)-1H-pyrazol-5-yl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide
CAS Number
1020172-07-9
Synonyms
  • DCC-2036
Molecular Formula
C30H28FN7O3
Formula Weight
553.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 1 mg/ml
λmax
251 nm
SMILES
CC(C)(C1=NN(C2=CC=C3C(C=CC=N3)=C2)C(N([H])C(N(C4=CC=C(C=C4F)OC5=CC(C(N(C)[H])=O)=NC=C5)[H])=O)=C1)C
InChi Code
InChI=1S/C30H28FN7O3/c1-30(2,3)26-17-27(38(37-26)19-7-9-23-18(14-19)6-5-12-33-23)36-29(40)35-24-10-8-20(15-22(24)31)41-21-11-13-34-25(16-21)28(39)32-4/h5-17H,1-4H3,(H,32,39)(H2,35,36,40)
InChi Key
WVXNSAVVKYZVOE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $396

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    Product Description

    Rebastinib is an orally bioavailable tyrosine kinase inhibitor that inhibits Abl1 (IC50 = 0.8 nM) as well as the gatekeeper mutant Abl1T315I (IC50 = 4 nM) and the activation loop mutant Abl1H396P.1 It also inhibits the Src family kinases Src, Lyn, Fgr, and Hck and the tyrosine kinases KDR, FLT3, and Tie2 at nanomolar concentrations. Rebastinib inhibits mutant Abl1T315I signaling and prolongs survival in a mouse Ba/F3 cell allograft model.1,2 Rebastinib also exhibits in vivo antineoplastic activity against cells with the T674I point mutation of FIP1-like-1-platelet-derived growth factor receptor α.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chan, W.W., Wise, S.C., Kaufman, M.D., et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell. 19(4), 556-568 (2011).

    2. Eide, C.A., Adrian, L.T., Tyner, J.W., et al. The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile. Cancer Res. 71(9), 3189-3195 (2011).

    3. Shen, Y., Shi, X., and Pan, J. The conformational control inhibitor of tyrosine kinases DCC-2036 is effective for imatinib-resistant cells expressing T674I FIP1L1-PDGFRα. PLoS One 8(8), e73059 (2013).