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Chemical Structure| 1632250-49-7 Chemical Structure| 1632250-49-7

Structure of PF-06446846
CAS No.: 1632250-49-7

Chemical Structure| 1632250-49-7

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PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling 80S ribosomes near codon regions.

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Product Details of PF-06446846

CAS No. :1632250-49-7
Formula : C22H20ClN7O
M.W : 433.89
SMILES Code : O=C(N(C1=NC=CC=C1Cl)[C@H]2CNCCC2)C3=CC=C(N4N=NC5=CC=CN=C54)C=C3
MDL No. :MFCD32182630
InChI Key :FDTXHWQFIXYHCL-QGZVFWFLSA-N
Pubchem ID :86271238

Safety of PF-06446846

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Huh7 cells 0.3 µM Overnight Inhibited PCSK9 secretion with an IC50 of 0.3 μM PLoS Biol. 2017 Mar 21;15(3):e2001882
HEK293T cells 4 µM 20 hours To test whether PF846 can selectively inhibit translation termination in cells Nat Commun. 2020 Oct 2;11(1):4941
HeLa cells 0.1 mM 23 minutes To investigate the mechanism of selective stalling of human ribosomes by PF846, results showed that PF846 selectively stalls translation of specific mRNAs. Nat Struct Mol Biol. 2019 Jun;26(6):501-509
HeLa cells 50 µM 23 minutes To assess the effects of mutations in the nascent-chain sequence on PF846-dependent inhibition of translation termination Nat Commun. 2020 Oct 2;11(1):4941
HeLa cells 50 µM 45 minutes Inhibited translation of PCSK9(1-35)-luciferase fusion constructs PLoS Biol. 2017 Mar 21;15(3):e2001882
JHOS2 cells 100 µM 48 hours Evaluate the effect of PF-06446846 on JHOS2 cell proliferation, showing 85% cell survival, indicating that PCSK9 plays a survival role in these cancer cells. Cancers (Basel). 2021 Jul 24;13(15):3727
OVCAR3cis cells 100 µM 48 hours Evaluate the effect of PF-06446846 on OVCAR3cis cell proliferation, showing significant inhibition at 100 μM concentration. Cancers (Basel). 2021 Jul 24;13(15):3727
OVCAR3 cells 100 µM 48 hours Evaluate the effect of PF-06446846 on OVCAR3 cell proliferation, showing significant inhibition at 100 μM concentration. Cancers (Basel). 2021 Jul 24;13(15):3727

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Sprague-Dawley rats Oral 5, 15, 50 mg/kg Once daily for 14 days Reduced plasma PCSK9 and total cholesterol levels PLoS Biol. 2017 Mar 21;15(3):e2001882

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.52mL

2.30mL

1.15mL

23.05mL

4.61mL

2.30mL

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