PF-06873600 Chemical Properties

Boiling point:

634.0±65.0 °C(Predicted)

Density 

1.47±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:15.0(Max Conc. mg/mL);31.81(Max Conc. mM)

form 

A solid

pka

14.69±0.40(Predicted)

color 

White to light yellow

InChIKey

QIEKHLDZKRQLLN-FOIQADDNSA-N

SMILES

C1(NC2CCN(S(C)(=O)=O)CC2)=NC=C2C=C(C(F)F)C(=O)N([C@@H]3CCC[C@]3(O)C)C2=N1

PF-06873600 Usage And Synthesis

Description

PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer.
PF-06873600 is an inhibitor of cyclin-dependent kinase 2 (CDK2), CDK4, and CDK6 with Ki values of 0.1, 1.2, and 0.1 nM, respectively. It also blocks the phosphorylation of retinoblastoma protein (RB1) and limits the proliferation of OVCAR-3 ovarian cancer cells with EC50s of 19 and 45 nM, respectively.

Uses

PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 has potential antineoplastic activity[1][2].

Mechanism of action

PF-06873600 is taken as a tablet by mouth. PF-06873600 is a cancer growth blocker targeting specific proteins called Cyclin-Dependent Kinase 2, 4, and 6 (CDK2/4/6). It works by stopping or preventing the action of these proteins, which stimulate cancer cells to grow and divide. PF-06873600 selectively targets, binds to, and inhibits the activity of CDKs. Inhibition of these kinases leads to cell cycle arrest, induction of apoptosis and inhibition of tumor cell proliferation. CDKs, ATP-dependent serine/threonine kinases that are essential regulators of cell cycle progression and cellular proliferation are frequently overexpressed in tumour cells.

IC 50

CDK2: 0.09 nM (Ki); CDK4: 0.13 nM (Ki); CDK6: 0.16 nM (Ki)

References

[1] US 2018/0044344 A1.
[2] NCI Drug Dictionary

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