CADD522

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CADD522 是一种有效的 runt 相关转录因子-2 (RUNX2)-DNA 结合抑制剂，IC50 为 10 nM，具有抗肿瘤活性CADD522 是一种有效的 runt 相关转录因子-2 (RUNX2)-DNA 结合抑制剂（IC50 为10 nM)，具有抗肿瘤活性。

CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM, with antitumor activity.CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding( IC50 of 10 nM), has antitumor activity.

Cell Viability Assay Cell Line:MDA-MB-468, MCF7, MCF10A, IEC-6, GES-1 and C2C12 cells Concentration:0-100 μM Incubation Time:24-72 h Result:Displayed a dose- and time-dependent cell growth inhibition over 72 h.Exhibited low cytotoxicity for normal cell growth.Cell Cycle Analysis Cell Line:MCF7, MDA-468 and MDA-231 cells Concentration:50 μM Incubation Time:72 h Result:Induced MDA-231 cells accumulated at the G1 and G2/M phase whereas MCF7 and MDA-468 cells were at the G1 phase.Cell Viability Assay Cell Line:MCF7, MCF7-tet-off cells Concentration:50 μM Incubation Time:8 daysResult:Dramatically decreased the size as well as the number of tumorspheres, and severely disrupted tumorspheres at day 4.Showed a relatively selective effect on BC cells (did not have a significant influence on mammosphere formation of the MCF10A non-malignant mammary epithelial cells).Cell Invasion Assay Cell Line:MCF7-tet-off (+Doxy), MCF7-tet-off (-Doxy) cells Concentration:50 μM Incubation Time:24 h Result:Almost abrogated the invasiveness of both MCF7-tet-off (+Doxy) and MCF7-tet-off (-Doxy) cells without cellular toxicity.Cell Viability Assay Cell Line:T47D-RUNX2 and T47D-Empty cells Concentration:2, 10, 25, 50, 100 μM Incubation Time:48 h Result:Resulted in a dramatic decrease of the promoter-luciferase (Luc) activities of RUNX2 downstream target genes such as MMP13 and VEGF (metastasis markers) and OC (osteogenesis marker).RT-PCRCell Line:T47D and MCF7 cells (ectopic expressing RUNX2)Concentration:50 μM Incubation Time:72 h Result:Significantly inhibited the mRNA level (RUNX2-mediated) of Glut-1 and LDHA.Western Blot Analysis Cell Line:T47D-RUNX2 and MCF7-RUNX2 cellsConcentration:50 μM Incubation Time:72 hResult:Enhanced both mRNA and protein expression of RUNX2.Western Blot Analysis Cell Line:MDA-468 and MDA-231 cells Concentration:50 μM Incubation Time:2, 4, 6 h Result:Increased RUNX2 stability by delaying protein degradation.Cell Viability Assay Cell Line:MCF7 and MDA-468 cells Concentration:50 μM Incubation Time:6 or 24 h Result:Increased the level of mitochondrial ROS, which was more evident in serum-free than serum-containing condition.Cell Viability Assay Cell Line:MDA-231 and MDA-468 cellsConcentration:50, 250, 2000 nM (for MDA-231); 500, 2000 nM (for MDA-468)Incubation Time:30 min Result:Inhibited the activity of A TP synthase.

Animal Model:Female mice (6-week-old; MMTV-PyMT transgenic model).Dosage:1, 5 and 20 mg/kg Administration:Intraperitoneal injection; twice a week for 45 days.Result:Delayed the onset of the tumors, delayed tumor development and reduced tumor burden in transgenic MMTV-PyMT mice.Reduced the tumor weight in mice.Animal Model:Female NOD scid gamma (NSG) mice and nude mice (TNBC-PDX Br-001 model). Dosage:10 mg/kg Administration:Intraperitoneal injection; twice a week for 11 days.Result:Significant decreased tumor volume and markedly inhibited expression of Ki-67.Inhibited experimental metastasis of BC cells in vivo.(did not significantly decrease body weight or influence the general health of animals).

MFCD00167693

Others

Other Targets

runt-related transcription factor-2 (RUNX2)-DNA

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199735-88-1

326.17

C15H13Cl2NO3

>98% (HPLC)

DMSO:245 mg/ml(751.14 mM; Need ultrasonic)

OC(=O)C1C2CC(C=C2)C1C(=O)Nc1ccc(Cl)c(Cl)c1

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(-20℃)

With Ice Pack

≥ 2 years