An inhibitor of Cdk2, Cdk4, and Cdk6
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PF-06873600

Item No. 35502

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one
CAS Number
2185857-97-8
Synonyms
  • PF-3600
Molecular Formula
C20H27F2N5O4S
Formula Weight
471.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 15 mg/ml
λmax
228, 350 nm
SMILES
O=C1N([C@@]2([H])[C@](O)(CCC2)C)C3=NC(NC4CCN(CC4)S(C)(=O)=O)=NC=C3C=C1C(F)F
InChi Code
InChI=1S/C20H27F2N5O4S/c1-20(29)7-3-4-15(20)27-17-12(10-14(16(21)22)18(27)28)11-23-19(25-17)24-13-5-8-26(9-6-13)32(2,30)31/h10-11,13,15-16,29H,3-9H2,1-2H3,(H,23,24,25)/t15-,20-/m1/s1
InChi Key
QIEKHLDZKRQLLN-FOIQADDNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $91

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    5 mg

    $313

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    10 mg

    $402

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    25 mg

    $667

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    Product Description

    PF-06873600 is an inhibitor of cyclin-dependent kinase 2 (Cdk2), Cdk4, and Cdk6 (Kis = 0.13, 1.25, and 0.11 nM, respectively).1 It is selective for these CDKs over Cdk1 and Cdk9 (Kis = 4.5 and 19.6 nM, respectively). PF-06873600 inhibits the phosphorylation of RB transcriptional corepressor 1 (RB1) in, and the proliferation of, OVCAR-3 ovarian cancer cells (EC50s = 19 and 45 nM, respectively). In vivo, PF-06873600 (30 mg/kg) reduces tumor volume in CTG-0464 and CTG-01912 non-small cell lung cancer (NSCLC) patient-derived xenograft (PDX) mouse models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Freeman-Cook, K.D., Hoffman, R.L., Behenna, D.C., et al. Discovery of PF-06873600, a CDK2/4/6 inhibitor for the treatment of cancer. J. Med. Chem. 64(13), 9056-9077 (2021).