An inhibitor of CK1δ and CK1ε
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SR 3029

Item No. 27048

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(6,7-difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(4-morpholinyl)-9H-purin-6-amine
CAS Number
1454585-06-8
Molecular Formula
C23H19F3N8O
Formula Weight
480.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/ml
λmax
231, 281 nm
SMILES
FC1=C(F)C(N2)=C(C=C1)N=C2CNC3=C4C(N(C5=CC=CC(F)=C5)C=N4)=NC(N6CCOCC6)=N3
InChi Code
InChI=1S/C23H19F3N8O/c24-13-2-1-3-14(10-13)34-12-28-20-21(31-23(32-22(20)34)33-6-8-35-9-7-33)27-11-17-29-16-5-4-15(25)18(26)19(16)30-17/h1-5,10,12H,6-9,11H2,(H,29,30)(H,27,31,32)
InChi Key
CEBMEQPREMCWOL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $95

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    10 mg

    $178

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    25 mg

    $284

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    Product Description

    SR 3029 is an inhibitor of casein kinase 1δ (CK1δ) and CK1ε (IC50s = 44 and 260 nM, respectively).1 It is selective for CK1δ and CK1ε over 438 kinases in a panel but also inhibits MYLK4, FLT3, Cdk4/cyclin D1, and MARK2 by greater than 90% at 10 µM. SR 3029 inhibits Cdk4/cyclin D1, Cdk4/cyclin D3, Cdk6/cyclin D1, Cdk6/cyclin D3, and FLT3 with IC50 values of 576, 368, 428, 427, and 3,000 nM, respectively. It inhibits proliferation of A375 human melanoma cells in vitro (EC50 = 86 nM). SR 3029 (20 mg/kg per day) reduces tumor growth and increases lifespan in MDA-MB-231 and MDA-MB-468 mouse xenograft models.2 It reduces the expression of the Wnt/β-catenin target CCND1 and decreases protein levels of nuclear β-catenin and cyclin D1 in mouse tumor tissue.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bibian, M., Rahaim, R.J., Choi, J.Y., et al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg. Med. Chem. Lett. 23(15), 4374-4380 (2013).

    2. Rosenberg, L.H., Lafitte, M., Quereda, V., et al. Therapeutic targeting of casein kinase 1δ in breast cancer. Sci. Transl. Med. 7(318), 318ra202 (2015).