A mutant EGFR inhibitor
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1,2,3,4-Tetrahydrostaurosporine

Item No. 29987

Technical Information
Formal Name
(9S,10R,11R,13R)-2,3,10,11,12,13,15,16,17,18-decahydro-10-methoxy-9-methyl-11-(methylamino)-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3′,2′,1′-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one
CAS Number
220038-19-7
Synonyms
  • AFN-941
Molecular Formula
C28H30N4O3
Formula Weight
Purity
≥95%
A solid
Acetone: Slightly solubleDMSO: Slightly soluble
SMILES
[H][C@]12N(C3=C4C5=C(CNC5=O)C6=C3N([C@](O2)(C)[C@H](OC)[C@H](NC)C1)C7=CC=CC=C76)C8=C4CCCC8
InChi Code
InChI=1S/C28H30N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h5,7,9,11,17,20,26,29H,4,6,8,10,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
InChi Key
KIZWKTROWIIMNN-FYTWVXJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    1,2,3,4-Tetrahydrostaurosporine is a derivative of staurosporine (Item No. 81590) and an inhibitor of mutant EGFR (IC50 = 74 nM for EGFRT790M).1 It is selective for EGFRT790M over wild-type EGFR (IC50 = 390 nM). It also binds to Janus kinase 3 (JAK3).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Song, X., Liu, X., and Ding, X. Staurosporine scaffold-based rational discovery of the wild-type sparing reversible inhibitors of EGFR T790M gatekeeper mutant in lung cancer with analog-sensitive kinase technology. J. Mol. Recognit. 30(4):e2590, (2017).

    2. Boggon, T.J., Li, Y., Manley, P.W., et alCrystal structure of the Jak3 kinase domain in complex with a staurosporine analog. Blood 106(3), 996-1002 (2005).