An inhibitor of Src kinases
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eCF506

Item No. 19959

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[4-amino-1-[2-[4-(dimethylamino)-1-piperidinyl]ethyl]-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]-carbamic acid, 1,1-dimethylethyl ester
CAS Number
1914078-41-3
Molecular Formula
C26H38N8O3
Formula Weight
510.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlEthanol: 15 mg/ml
λmax
251, 268, 300 nm
SMILES
COC1=CC(C2=NN(CCN3CCC(N(C)C)CC3)C4=NC=NC(N)=C42)=CC=C1NC(OC(C)(C)C)=O
InChi Code
InChI=1S/C26H38N8O3/c1-26(2,3)37-25(35)30-19-8-7-17(15-20(19)36-6)22-21-23(27)28-16-29-24(21)34(31-22)14-13-33-11-9-18(10-12-33)32(4)5/h7-8,15-16,18H,9-14H2,1-6H3,(H,30,35)(H2,27,28,29)
InChi Key
GMPQGWXPDRNCBL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $186

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    10 mg

    $351

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    25 mg

    $583

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    Product Description

    eCF506 is an inhibitor of Src kinases (IC50s = <0.5, 2.1, <0.5 nM for Src, Fyn, and Yes, respectively).1 It is selective for Src kinases over Abl (IC50 = 479 nM), as well as KIT, mTOR, PDGFRα, and RET (IC50s = >100 µM for all). eCF506 completely inhibits phosphorylation of Src and FAK, a downstream Src substrate, in MCF-7 and MDA-MB-231 cells when used at a concentration of 100 nM. It also inhibits proliferation of MCF-7 cells (EC50 = 9 nM) and induces apoptosis. eCF506 (50 mg/kg per day) reduces levels of activated Src kinase in tumor tissue in an HCT116 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fraser, C., Dawson, J.C., Dowling, R., et al. Rapid discovery and structure-activity relationships of pyrazolopyrimidines that potently suppress breast cancer cell growth via SRC kinase inhibition with exceptional selectivity over ABL kinase. J. Med. Chem. 59(10), 4697-4710 (2016).