VC KX-01 Total Src p-Y416 Src Supplementary Figure S1. KX-01 at low dose inhibited phosphorylation of Src in MDA-MB-231 xenografts.

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VC KX-01 Total Src p-Y416 Src Supplementary Figure S1. KX-01 at low dose inhibited phosphorylation of Src in MDA-MB-231 xenografts.

ER m-RNA expression in PDX tumors * * Supplementary Figure S2. Effect of KX-01 on ERα mRNA expression in Patient Derived Xenograft (PDX) tumors.

MDA-MB-231 tumor c-myc Cyclin D1 PS2 GAPDH MCF-7 VC TAM KX-01 TAM+KX-01 c-myc Cyclin D1 PS2 GAPDH Supplementary Figure S3. Effect of KX-01 and tamoxifen on ERα regulated proteins c-myc, cyclin D1 and pS2 in MDA-MB-231 tumor lysates by Western blot analysis.

Positive control for TUNEL DAPI VC TAM TUNEL DAPI TUNEL DAPI TUNEL DAPI KX-01 KX-01 + TAM * * Supplementary Figure S4. TUNEL immunofluorescence microscopy on MDA-MB-231 tumor sections from mice treated with VC, TAM, KX-01, KX-01 + TAM.

A. ERα immunostaining Vehicle control KX-01 1mg/kg b.wt PR immunostaining Vehicle control KX-01 1mg/kg b.wt B. MDA-MB-157 tumor xenograft Vehicle control Tamoxifen 5mg pellet (60 day release) KX-01 1mg/kg b.wt KX-01 + Tamoxifen Supplementary Figure S5. Effect of KX-01and tamoxifen co-treatment on growth of MDA-MB-157 breast tumor xenografts.

TUNEL VC DAPI TUNEL TAM DAPI KX-01 KX-01 + TAM * * Supplementary Figure S6. TUNEL immunofluorescence microscopy on MDA-MB-157 tumor sections from mice treated with VC, TAM, KX-01, KX-01 + TAM.

B ERα expression at day 30 in MDA-MB-231 tumors A MDA-MB-231 tumor volume KX-01 (day 1-14); VC (day 15-30) KX-01 (day 1-14); TAM (day 15-30) B ERα expression at day 30 in MDA-MB-231 tumors KX-01 (day 1-14); VC (day 15-30) KX-01 (day 1-14); TAM (day 15-30) ERα C ERα expression MCF-7 tumor (positive control) ERα Supplementary Figure S7. Effect of KX-01 withdrawal on ERα expression and tamoxifen sensitivity in MDA-MB-231 tumors.

MDA-MB-231 tumor ERα E-cad GAPDH MCF-7 VC TAM KX-01 TAM+KX-01 ERα E-cad GAPDH Supplementary Figure S8. Effect of KX-01 on ERα and E-cadherin protein expression in MDA-MB-231 xenografts measured by Western blot analysis of tumor lysates.

Supplementary Figure S9 Supplementary Figure S9. Effect of KX-01 on histone deacetylases (HDACs) activity in MDA-MB-231 tumors.

Supplementary Figure S10. Low dose KX-01 had no effect on microtubule Tubulin DAPI VC TAM 5 mg pellet (60 day release) KX-01 (1mg/kg/BID) KX-01 (1mg/kg/BID)+TAM KX-01 (5mg/kg/BID) Supplementary Figure S10. Low dose KX-01 had no effect on microtubule formation in MDA-MB-231 tumors.

ERα GAPDH ERα m-RNA expression in TNBC cell lines after treatment of with KX-01 25 nM for 96 h MCF-7 MDA-MB-231 MDA-MB-468 MDA-MB 157 VC KX-01 Supplementary Figure S11. ERα mRNA expression induced by KX-01 in MDA-MB-231, MDA-MB-468 and MDA-MB-157 triple negative breast cancer cells.