An orally available inhibitor of ALK
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CH5424802

Item No. 18516

Technical Information
Formal Name
9-ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
CAS Number
1256580-46-7
Synonyms
  • Alectinib
  • RO5424802
Molecular Formula
C30H34N4O2
Formula Weight
Purity
≥95%
A crystalline solid
DMF: 3 mg/mLDMF:PBS(pH7.2) (1:2): 0.3 mg/mL
λmax
232, 262, 281, 337 nm
SMILES
CCC1=CC2=C(C(C)(C)C(NC3=C4C=CC(C#N)=C3)=C4C2=O)C=C1N(CC5)CCC5N6CCOCC6
InChi Code
InChI=1S/C30H34N4O2/c1-4-20-16-23-24(17-26(20)34-9-7-21(8-10-34)33-11-13-36-14-12-33)30(2,3)29-27(28(23)35)22-6-5-19(18-31)15-25(22)32-29/h5-6,15-17,21,32H,4,7-14H2,1-3H3
InChi Key
KDGFLJKFZUIJMX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    CH5424802 is an ATP-competitive inhibitor of ALK (IC50 = 1.9 nM) that also inhibits F1174L, R1275Q, and L1196M mutants of ALK (IC50s = 1.0, 3.5, and 1.6 nM, respectively).1,2 It shows more than 500-fold selectivity for ALK over a panel of 24 other kinases.1 CH5424802 is orally available and inhibits the growth of tumors in mouse xenograft models of nonsmall cell lung cancer and anaplastic large-cell lymphoma.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sakamoto, H., Tskaguchi, T., Hiroshima, S., et alCH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell 19, 679-690 (2011).

    2. Awad, M.M., and Shaw, A.T. ALK inhibitors in non-small cell lung cancer: Crizotinib and beyond. Clin. Adv. Hematol. Oncol. 12(7), 429-439 (2014).