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. 2021 Nov 12;126(7):994–1003. doi: 10.1038/s41416-021-01616-2

Table 2.

CSNK2 inhibition in xenograft models sorted by cancer type.

Cancer Type Engrafted Cell Line : Host Intervention Results (Control vs Intervention) Reference (Appendix 2)
Bladder EJ bladder cancer cells: nude mice (female) EJ cells with either CSNK2A1 shRNA or control shRNA engrafted into nude mice Tumour volume at 21 days: 425 mm3 vs 175 mm3 (p < 0.01) 237
Bone 143B cells: nude mice CX4945 150 mg/kg daily oral Survival lower (p < 0.05) and tumour size greater (p < 0.05) in control compared to CX4945 at study endpoints 193
Brain U87-Luc cells: nude mice (female) TBB 10 mg/kg daily intra-peritoneal Intracranial luc fluorescence signal on day 11: 109.5 vs 108.5 (p < 0.01) 29
Brain U3054MG cells: SCID or nude mice (female) CX4945 75 mg/kg daily oral Growth at 68 days: no significant difference between CX4945 and control 147
Brain U87MG cells: nude mice TBB 10 mg/kg q48 h intra-peritoneal Tumour mass at 25 days: 650 mg vs 125 mg (p < 0.05) 42
Brain

LN229 cells: nude mice

U87MG cells: nude mice

Anti-sense CSNK2A1 + cetuximab nanobioconjugate intra-venous twice per week for 3 weeks

LN229—survival: 37 days vs 70 days (p < 0.001)

U87MG—survival: 34 days vs 48 days (p < 0.05)

31
Brain U87MG cells: SCID mice Engraftment of U87MG cells with CSNK2A knockdown via induced CSNK2A shRNA Survival: 20 days vs >40 days (p < 0.0009) 137
Brain X1046 cells: nude mice CX4945 75 mg/kg BID oral for 28 days starting at day 5 Survival: 38 days vs 59 days 239
Breast MDA-MB-231 cells: mice Tenfibgen siRNA-CSNK2 0.01 mg/kg by tail vein injection Tumour volume on day 10 relative to day 0: 2.1× vs 1.4× (p = 0.026) 200
Breast MDA-MB-231 cells: nude mice (female)

Tenfibgen siRNA-CSNK2 0.01 mg/kg on day 1, 4, 7 by

tail vein injection

Tumour volume on day 10 relative to day 0: 2.05× vs 1.35× (p < 0.05) 97
Breast BT-474 cells: nude mice (female) CX4945 75 mg/kg BID oral Tumour volume at 30 days: 650 mm3 vs 190 mm3 (p < 0.001) 183
Cervical SiHa cells: nude mice CIGB-300 200ug daily intra-tumour for 5 days Tumour volume at 21 days: 175 mm3 vs 60 mm3 245
Cervical SiHa cells: nude mice (male and female) CIGB-300 200ug daily intra-tumour for 5 days

Survival (median)—female: 33 days vs 59.0 days

Survival (median)—male: 40.0 days vs 44.5 days

150
Head and neck UM-SCC1 cells: SCID mice (female) CX4945 75 mg/kg BID oral Tumour volume at 25 days: 1000 mm3 vs 650 mm3 (p < 0.05) 13
Head and neck FaDu cells: nude mice Tenfibgen s50 RNAi-CSNK2 10 mg/kg twice q48h by tail vein injection Tumour volume at 35 days: 1075 mm3 vs 75 mm3 (p < 0.0001) 204
Head and neck

(A) UM-SCC 11 A cells: SCID mice (male)

(B) FaDu cells: nude mice (female)

(A) Tenfibgen nanocapsules with anti-CSNK2A1/A2 at 10 ug/kg intra-peritoneal q3days.

(B) Tenfibgen nanocapsules with anti-CSNK2A1/A2 at 10 ug/kg IV q48 h for 2 doses

(A) Tumour volume at 7 days: 620 mm3 vs 250 mm3 (p < 0.01)

(B) Tumour volume at 7 days: 180 mm3 vs 50 mm3 (p < 0.01)

18
Leukemia—CLL MO1043 cells: nude mice CX4945 75 mg/kg BID oral Tumour volume at 13 days: 450 mm3 vs 225 mm3 (p < 0.001) 129
Leukemia—CLL MO1043 cells: nude mice CIGB-300 20 mg/kg intra-peritoneal for 5 days plus 2 days rest, then repeated Tumour volume at 15 days: 1200 mm3 vs 600 mm3 (p < 0.001) 128
Liver HepG2 cells: NMRI nude mice (male) DMAT 500 ug/kg daily intra-peritoneal Tumour volume at 10 days: 600 mm3 vs 200 mm3 (P < 0.05) 169
Lung H-125 cells: nude mice (female) P15-Tat (ie CIGB-300) 10 mg/kg intra-peritoneal for 5 days Survival: 24 days vs 41 days (p = 0.0002) 151
Ovarian SKOV3 EOC cells: nude mice CX4945 75 mg/kg daily oral Tumour volume at 21 days: 400 mm3 vs 180 mm3 (p < 0.01) 25
Ovarian IGORV-1 cells: nude mice (female) CX4945 75 mg/kg daily oral Proliferative index at 42 days: 37% vs 16% (p < 0.001). Vascular tumur area at 42 days: 28% vs 14% (p < 0.001). 99
Ovarian A2780 cells: nude mice (female) CX4945 100 mg/kg BID oral (days 2, 5, 8 and 11) and/or gemcitabine 30 mg/kg intra-peritoneal every 3 days (days 1, 4, 7 and 10)

Time to reach tumour volume of 2000 mm3: 11 days (control),

13 days (CX4945), 37 days (gemcitabine), 51 days (combination)

182
Pancreatic BxPC-3 cells: nude mice (female) CX4945 75 mg/kg BID oral Tumour volume at 35 days: 850 mm3 vs 190 mm3 (p < 0.001) 183
Pancreatic MiaPaCa2 cells: nude mice (male) siRNA PAK7 ± siRNA-CSNK2 q3days intra-peritoneal Tumour volume at 21 days: 900 mm3 (control), 500 mm3 (PAK7) (p < 0.05), 230 mm3 (PAK7 + CSNK2) (p < 0.05) 57
Prostate 22Rv1 cells: SCID mice (male) Tenfibgen RNAi-CSNK2 0.02 mg/kg by tail vein injection on days 1, 4, 7 Tumour weight on day 8: 1.1 g vs 0.35 g 201
Prostate PC3-LN4 cells: mice Tenfibgen RNAi-CSNK2 0.01 mg/kg by tail vein injection Tumour volume on day 10 relative to day 0: 12.2× vs 5.2× (p = 0.005) 200
Prostate PC3-LN4 cells: nude mice (male) Tenfibgen RNAi-CSNK2 0.01 mg/kg by tail vein injection on days 1, 4, 7

Tumour volume fold change relative to day 0, at day 10:

12× vs 5× (p = 0.05)

3
Prostate PC3-LN4: nude mice (male) Tenfibgen RNAi-CSNK2 33 ng/kg intra-peritoneal twice, given 24 h apart

Tumour volume relative to control at 13 days: 100% vs 25%

(p = 0.011)

203
Prostate PC3-LN4: nude mice (male) DMAT 500ug/kg daily intra-peritoneal for 6 days Ki-67 proliferation index on day 7: 60% vs 30% (p < 0.002) 202
Prostate PC3 cells: nude mice TBB—dosing regimen not disclosed Tumour volume at 35 days: 325 mm3 vs 125 mm3 (p < 0.001) 232
Prostate PC3 cells: nude mice CX4945 75 mg/kg BID oral Tumour volume at 25 days: 775 mm3 vs 200 mm3 153
Prostate PC3-LN4: nude mice (male) Anti-sense CSNK2 16.5 ug/kg daily for 4 doses intra-peritoneal Tumour mass at 13 days: 1000 mg vs 300 mg (p < 0.05) 199
Prostate PC3-LN4: nude mice (male) Anti-sense CSNK2A1 20 ug once intra-tumour Tumour size at 8 days: 4.25 mm vs 0.0 mm 187

Representative experiments from each publication identified in this systematic review were highlighted. For each, the host organism (and sex, if specified) alongside the cancer cell line engrafted into the host was listed. Corresponding interventions were summarised, with results from the control and intervention groups recorded thereafter (absolute values were either quoted directly or their closest approximation listed). Statistical significance was provided when available. Numbered citations for all studies listed corresponded with references in Appendix 2 of the Supplementary Information.