A selective Cdk inhibitor
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R547

Item No. 17905

Technical Information
Formal Name
[4-amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxyphenyl)-methanone
CAS Number
741713-40-6
Synonyms
  • Ro 4584820
Molecular Formula
C18H21F2N5O4S
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 15mg/mlDMSO: 15 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml
λmax
221, 277, 316 nm
SMILES
O=C(C1=C(N)N=C(NC2CCN(S(C)(=O)=O)CC2)N=C1)C3=C(F)C(F)=CC=C3OC
InChi Code
InChI=1S/C18H21F2N5O4S/c1-29-13-4-3-12(19)15(20)14(13)16(26)11-9-22-18(24-17(11)21)23-10-5-7-25(8-6-10)30(2,27)28/h3-4,9-10H,5-8H2,1-2H3,(H3,21,22,23,24)
InChi Key
JRNJNYBQQYBCLE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    R547 is a diaminopyrimidine compound that inhibits Cdk1/cyclin B, Cdk2/cyclin E, and Cdk4/cyclin D1 (Kis = 1-3 nM).1 It is inactive against a panel of more than 120 unrelated kinases (Kis > 5 µM).1 R547 inhibits tumor cell proliferation (IC50s ≤ 0.6 µM in vitro), inducing cell cycle arrest at G1 and G2 phases and apoptosis as well as reducing phosphorylation of the retinoblastoma protein.1 It also demonstrates antitumor activity in vivo in various human tumor xenograft models.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. DePinto, W., Chu, X.J., Yin, X., et alIn vitro and in vivo activity of R547: A potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials. Mol. Cancer Ther. 5(11), 2644-2658 (2006).