An Axl kinase inhibitor
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R428

Item No. 21523

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5Hbenzocyclohepten-2-yl]-1H-1,2,4-triazole-3,5-diamine
CAS Number
1037624-75-1
Synonyms
  • Bemcentinib
  • BGB 324
Molecular Formula
C30H34N8
Formula Weight
506.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: >5 mg/ml
λmax
258, 317 nm
SMILES
NC1=NC(NC2=CC=C3C(CC[C@@H](N4CCCC4)CC3)=C2)=NN1C5=NN=C(C(C=CC=C6)=C6CCC7)C7=C5
InChi Code
InChI=1S/C30H34N8/c31-29-33-30(32-24-13-10-20-11-14-25(15-12-22(20)18-24)37-16-3-4-17-37)36-38(29)27-19-23-8-5-7-21-6-1-2-9-26(21)28(23)35-34-27/h1-2,6,9-10,13,18-19,25H,3-5,7-8,11-12,14-17H2,(H3,31,32,33,36)/t25-/m0/s1
InChi Key
KXMZDGSRSGHMMK-VWLOTQADSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $83

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    10 mg

    $152

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    25 mg

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    Product Description

    R428 is a small molecule inhibitor of Axl kinase, both in an in vitro biochemical assay and in a cell-based assay using phosphorylation of Ser473 on Akt as the readout (EC50s = 14 nM for both).1 It is orally bioavailable, blocks angiogenesis in corneal micropocket and tumor models, and reduces metastatic burden while extending survival in mouse models of breast cancer metastasis.1 R428 synergizes with cisplatin (Item No. 13119) to enhance suppression of liver micrometastasis.1 R428 is used to study the role of Axl kinase signaling in cancer, cellular senescence, and Zika virus infection.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Holland, S.J., Pan, A., Franci, C.R., et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 70(4), 1544-1554 (2010).

    2. Brand, T.M., Iida, M., Stein, A.P., et al. AXL is a logical molecular target in head and neck squamous cell carcinoma. Clin. Cancer Res. 21(11), 2601-2612 (2015).

    3. Jin, C.-w., Wang, H., Chen, Y.-q., et al. Gas6 delays senescence in vascular smooth muscle cells through the PI3K/ Akt/FoxO signaling pathway. Cell. Physiol. Biochem. 35(3), 1151-1166 (2015).

    4. Meertens, L., Labeau, A., Dejarnac, O., et al. Axl mediates ZIKA virus entry in human glial cells and modulates innate immune responses. Cell Rep. 18(2), 324-333 (2017).