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Supplementary Figure S1 AB
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Supplementary Table S1 Clinical exposure for palbociclib, fulvestrant and chemotherapeutic agents used in this study.
Palbociclib (1)* Paclitaxel (2)* Doxorubicin (3)* Fulvestrant (4)*
Clinical Dose 125 mg 175 mg/m2 60 mg/m2 500 mg/5ml
Cmax 202 nM 0.43 µM 1.16 µM 46 nM
Cave calculation 144 nM 0.078 µM 0.25 µM 30 nM
based on AUC (AUC 0-24hr 1982 ng.h/ml) (AUC 0-120hr 7993ng.h/ml) (AUC 0-24hr 358ng.h/ml) (AUC 0-15day 13100 ng.hr/ml)
* Numbers in parenthesis indicate reference number.
Supplementary Table S2. Cell cycle analysis in human bone marrow mononuclear cells treated with palbociclib for 4 days.
Dead Cell G1 Phase S Phase G2/M Phase
Vehicle 6.25% (± 0.59%) 53.96% (± 2.33%) 27.93% (± 0.98%) 11.75% (± 1.91%)
Palbociclib 0.1uM 4.32% (± 0.84%) 60.98% (± 3.32%) 20.61% (± 0.84%) 13.19% (± 1.72%)
Palbociclib 0.3uM 4.66% (± 0.14%) 67.4% (± 2.04%) 16.10% (± 1.49%) 7.04% (± 0.39%)
Palbociclib 1uM 4.68% (± 1.17%) 79.23% (± 1.17%) 9.99% (± 2.59%) 4.55% (± 0.73%)
Supplementary Figure S1
A B
Supplementary Figure S2
Supplementary Figure S3
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Human M
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MCF-70.0
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0.2
0.3
0.4
Rela
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Gen
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Supplementary Figure S4