cell culture human tnbc mda mb 231 cells  (ATCC)

Journal: Molecular cancer therapeutics

Article Title: First-in-class phosphorylated-p68 inhibitor RX-5902 inhibits β-catenin signaling and demonstrates anti-tumor activity in triple-negative breast cancer

doi: 10.1158/1535-7163.MCT-18-1334

Figure Lengend Snippet: (A) Flow-cytometric analysis of cell-cycle distribution in two sensitive (MDA-MB-231 and HCT1806) and two resistant (MDA-MB-436 and CAL-120) cell lines exposed to RX-5902 for 24 hours. (B) Representative graphs for a sensitive (HCC1806) and a resistant (CAL-120) cell line treated with 100 nM RX-5902 or no drug control demonstrating cellular fractions in G1, G2/M and aneuploidy. (C) Indicated cell lines were treated with RX-5902 (0-100 nM) for 72 hours and apoptosis was assessed using the Incucyte Caspase 3/7 Green apoptosis assay with live cell microscopy. S; sensitive to RX-5902, R; resistant to RX-5902, ND; no drug control. *p<0.05, **p<0.01, ****p<0.0001,

Article Snippet: Cell lines and tissue culture Human TNBC cell lines MDA-MB-231, MDA-MB-436, MDA-MB-157, HCC1806, HCC1937, Hs578T, HCC38, BT549, HCC1187, and HCC1395 were obtained from American Type Culture Collection (ATCC, Manassas, VA).

Techniques: Apoptosis Assay, Microscopy

Journal: Molecular cancer therapeutics

Article Title: First-in-class phosphorylated-p68 inhibitor RX-5902 inhibits β-catenin signaling and demonstrates anti-tumor activity in triple-negative breast cancer

doi: 10.1158/1535-7163.MCT-18-1334

Figure Lengend Snippet: (A) MDA-MB-231, CAL-120, MDA-MB-436 and MCF-10A cells were treated with RX-5902 100 nM for 24 hours and immunoblotting was performed for MCL-1, phosphorylated p68, p68 and actin. Additionally, nuclear and cytoplasmic extract isolation was performed. Immunoblotting was performed for β-catenin and actin. (B) Quantification of immunoblots for nuclear β-catenin and MCL-1 normalized to actin and no drug control. (C) TNBC cell lines sensitive to RX-5902 (Cal-51, HCC-1806 and MDA-MB-468) were treated with RX-5902 and immunoblotting was performed for MCL-1 and actin. (D) Quantification of immunoblots for MCL-1. *p<0.05, ****p<0.0001.

Article Snippet: Cell lines and tissue culture Human TNBC cell lines MDA-MB-231, MDA-MB-436, MDA-MB-157, HCC1806, HCC1937, Hs578T, HCC38, BT549, HCC1187, and HCC1395 were obtained from American Type Culture Collection (ATCC, Manassas, VA).

Techniques: Western Blot, Isolation

Journal: Molecular cancer therapeutics

Article Title: First-in-class phosphorylated-p68 inhibitor RX-5902 inhibits β-catenin signaling and demonstrates anti-tumor activity in triple-negative breast cancer

doi: 10.1158/1535-7163.MCT-18-1334

Figure Lengend Snippet: (A) Effect of RX-5902 administered once weekly in the MDA-MB-231 xenograft model. Animals were randomized to treatment with vehicle, nab-paclitaxel 5 mg/kg IV twice a week × 3, RX-5902 160 mg/kg via oral gavage once weekly × 3, RX-5902 320 mg/kg once weekly × 3 or RX-5902 600 mg/kg once weekly × 3. Nab-paclitaxel was used as a chemotherapy control. Tumor growth inhibition (TGI) RX-5902 160 mg/kg 55.7%, 320 mg/kg 80.29% and 600 mg/kg 94.58%, p < 0.001. TGI nab-paclitaxel 45%. B) Immunoblots performed using protein isolated from tumor tissue obtained pre and 24h post RX-5902. Three mice were included in each group. Immunoblotting was performed for p-p68, C-myc, Cyclin D1, β-catenin and actin. C) Based on observed toxicity in the ongoing Phase I dose escalation study, the effect of lower dose RX-5902 5 days on 2 days off was investigated in the MDA-MB-231 xenograft model. TGI RX-5902 15 mg/kg 45%, 30 mg/kg 58% and 60 mg/kg 72%, p < 0.001. D) Plasma concentration-time curve after a single dose of RX-5902 15 mg/kg, 30 mg/kg or 60 mg/kg in thenMDA-MB-231 xenograft model in nude mice. E) Tumor concentration-time curve after a single dose of RX-5902 15 mg/kg, 30 mg/kg or 60 mg/kg in the MDA-MB-231 xenograft model in nude mice.

Article Snippet: Cell lines and tissue culture Human TNBC cell lines MDA-MB-231, MDA-MB-436, MDA-MB-157, HCC1806, HCC1937, Hs578T, HCC38, BT549, HCC1187, and HCC1395 were obtained from American Type Culture Collection (ATCC, Manassas, VA).

Techniques: Inhibition, Western Blot, Isolation, Concentration Assay