An inhibitor of cancer stem cells
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Amcasertib

Item No. 22980

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(diethylamino)ethyl]-5-[[1,2-dihydro-2-oxo-5-(2-phenyl-4-thiazolyl)-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
CAS Number
1129403-56-0
Synonyms
  • BBI503
Molecular Formula
C31H33N5O2S
Formula Weight
539.7
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS(pH7.2) (1:2): 0.33 mg/ml
λmax
247, 307, 410 nm
SMILES
CC1=C(C(NCCN(CC)CC)=O)C(C)=C(/C=C2C(C=C(C3=CSC(C4=CC=CC=C4)=N3)C=C5)=C5NC\2=O)N1
InChi Code
InChI=1S/C31H33N5O2S/c1-5-36(6-2)15-14-32-30(38)28-19(3)26(33-20(28)4)17-24-23-16-22(12-13-25(23)34-29(24)37)27-18-39-31(35-27)21-10-8-7-9-11-21/h7-13,16-18,33H,5-6,14-15H2,1-4H3,(H,32,38)(H,34,37)/b24-17+
InChi Key
QDWKGEFGLQMDAM-JJIBRWJFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $95

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    5 mg

    $439

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    10 mg

    $601

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    Cayman Chemical
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    Product Description

    Amcasertib is an inhibitor of cancer stem cells (CSCs).1 It inhibits the growth of HT-29 and MDA-MB-231 cancer cells (IC50s = 100-250 nM for both) and exhibits a 2-fold increase in potency for a population of SW480 cells enriched for CSCs. Amcasertib reduces spherogenesis of CD44+-enriched FaDu cells. Oral administration of amcasertib (100 mg/kg) reduces tumor growth in PC3, HepG2, FaDu, and MKN45 mouse xenograft models. Amcasertib also inhibits EGFR, C-MET, HER2, and PDGFRα in vitro without reducing global tyrosine kinase activity.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, C.J., Liu, J.-F., Li, W., et al. Compositions of kinase inhibitors and their use for treatment of cancer and other diseases related to kinases. (2009).