sti-571/gleevec/glivec/imatinib mesylate  (Novartis)

Journal: Oncotarget

Article Title: The new allosteric inhibitor asciminib is susceptible to resistance mediated by ABCB1 and ABCG2 overexpression in vitro

doi: 10.18632/oncotarget.24393

Figure Lengend Snippet: K562 10 μM asciminib cells were cultured for 72 h in increasing concentrations of asciminib in the absence and presence of 1 μM imatinib, 2 μM imatinib and 150 nM nilotinib. K562 control cells were cultured in proportionately less concentrations of TKI. The concentration of asciminib required to kill 50% of cells (LD50 asciminib ) was determined by Annexin V/7-AAD staining. Data represent the mean of at least 3 independent experiments. Analyses were performed using unpaired Student’s t -test (Welch’s correction was applied for data groups with unequal SD). Statistical analyses compared the LD50 asciminib in K562 10 μM asciminib vs K562 control cells (asterisks) and also the LD50 asciminib in K562 control/K562 10 μM asciminib when asciminib was used as a single agent vs asciminib used in combination with the specified concentrations of imatinib and nilotinib (hashes). Statistically significant alterations in LD50 asciminib are indicated ( * p < 0.05, *** p < 0.01, *** p < 0.001). Error bars represent SEM. IM = imatinib. NIL = nilotinib.

Article Snippet: Imatinib mesylate (imatinib; Glivec; formerly STI-571), Nilotinib (Tasigna; formerly AMN107) and asciminib were provided by Novartis Pharmaceuticals (Basel, Switzerland).

Techniques: Cell Culture, Control, Concentration Assay, Staining

Journal: Biomolecular Detection and Quantification

Article Title: Molecular techniques for the personalised management of patients with chronic myeloid leukaemia

doi: 10.1016/j.bdq.2017.01.001

Figure Lengend Snippet: TKI resistant BCR-ABL1 TKD mutations.

Article Snippet: Imatinib (Gleevec/Glivec or STI-571) was the first TKI identified by Novartis in high-throughput screens for TKIs.

Techniques: Mutagenesis

Journal: Journal of Reproduction & Infertility

Article Title: The Effects of Imatinib Mesylate on Cellular Viability, Platelet Derived Growth Factor and Stem Cell Factor in Mouse Testicular Normal Leydig Cells

doi:

Figure Lengend Snippet: Cellular viability in leydig cells treated with increasing concentrations of imatinib on different days. In all days of experiments, cellular viability decreased as drug concentration increased. Data represent mean values±SD of three replicates in each subgroup. Mean values were compared using ANOVA. *P<0.05, **p<0.01 according to Tukey’s post hoc tests

Article Snippet: Imatinib mesylate (Glivec®, STI 571; Novartis Pharma, Switzerland), an antitumor agent has been widely used to treat multiple cancers, most notably Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia and gastrointestinal stromal tumors.

Techniques: Concentration Assay

Journal: Journal of Reproduction & Infertility

Article Title: The Effects of Imatinib Mesylate on Cellular Viability, Platelet Derived Growth Factor and Stem Cell Factor in Mouse Testicular Normal Leydig Cells

doi:

Figure Lengend Snippet: PDGF levels in leydig cells treated with increasing concentrations of imatinib on different days. On days 4 and 6, PDGF levels increased as drug concentration increased. Data represent mean values±SD of three replicates in all subgroups. Mean values were compared using ANOVA. *P<0.05 according to Tukey’s post hoc tests

Article Snippet: Imatinib mesylate (Glivec®, STI 571; Novartis Pharma, Switzerland), an antitumor agent has been widely used to treat multiple cancers, most notably Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia and gastrointestinal stromal tumors.

Techniques: Concentration Assay

Journal: Journal of Reproduction & Infertility

Article Title: The Effects of Imatinib Mesylate on Cellular Viability, Platelet Derived Growth Factor and Stem Cell Factor in Mouse Testicular Normal Leydig Cells

doi:

Figure Lengend Snippet: SCF levels in leydig cells treated with increasing concentrations of imatinib on different days

Article Snippet: Imatinib mesylate (Glivec®, STI 571; Novartis Pharma, Switzerland), an antitumor agent has been widely used to treat multiple cancers, most notably Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia and gastrointestinal stromal tumors.

Techniques: Concentration Assay

Journal: Journal of molecular histology

Article Title: c-Abl mediates angiotensin II-induced apoptosis in podocytes

doi: 10.1007/s10735-013-9505-8

Figure Lengend Snippet: Ang II induced podocyte apoptosis in vivo and in vitro. (A) Apoptotic podocytes of rat kidneys were assessed by transmission electron microscopic analysis in different groups. (a) normal saline infused group on day 14; (b) Ang II infused group on day 14; (c) Ang II + STI-571 group on day 14; (d) normal saline infused group on day 28; (e) Ang II infused group on day 28; (f) Ang II + STI-571 group on day 28. Enriched nuclear euchromatin indicate apoptotic podocytes. Original magnification ×12 000, scale bars, 1μm. (n = 6). (B) Apoptotic podocytes of rat kidneys were assessed by TUNEL staining in different groups. (a) normal saline infused group on day 14; (b) Ang II infused group on day 14; (c) Ang II + STI-571 group on day 14; (d) normal saline infused group on day 28; (e) Ang II infused group on day 28; (f) Ang II + STI-571 group on day 28. Black arrows indicate apoptotic podocytes in Ang II-infused rats. *P < 0.05 versus control group at the same time point, #P < 0.05 versus Ang II infused group at the same time point, scale bars, 100μm. (n = 6). (C) Apoptotic cells were assessed by Hoechst-33342 staining in cultured podocyte stimulated by Ang II (10-8mol/L) with or without c-Abl inhibitor (Src-I1) at various time points. Original magnification ×400. *P < 0.05 versus 0h of Ang II, #P < 0.05 versus Ang II-treated podocytes at 6h, scale bars, 10μm.(n=3) (D) One representative experiment (percentage of apoptotic podocytes in the right 2 quadrants) was indicated by flow cytometry.

Article Snippet: Embedded with osmotic mini-pump (Alzet model 2002 or 2004, CA), rats were randomly subjected to normal saline infusion, or Ang II infusion at 400 ng/kg/min, or Ang II at 400 ng/kg/min + STI-571 (Glivec, Novartis, Switzerland) at 50 mg/kg/day by means of intragastric administration for 14 or 28 days.

Techniques: In Vivo, In Vitro, Transmission Assay, TUNEL Assay, Staining, Cell Culture, Flow Cytometry

Journal: Journal of molecular histology

Article Title: c-Abl mediates angiotensin II-induced apoptosis in podocytes

doi: 10.1007/s10735-013-9505-8

Figure Lengend Snippet: Ang II increased c-Abl expression in kidney and cultured podocytes. (A and B): Immunohistochemical staining detection of glomerular c-Abl expression in different groups. (a) normal saline infused group on day 14; (b) Ang II infused group on day 14; (c) Ang II + STI-571 group on day 14; (d) normal saline infused group on day 28; (e) Ang II infused group on day 28; (f) Ang II + STI-571 group on day 28. (g) negative control group; (h) human normal renal tissue adjacent to kidney tumor, scar bar, 10μm. (n = 6). *P < 0.05 versus control group at the same time point, #P < 0.05 versus Ang II infused group at the same time point. (C) and (D) Real-time PCR and western blot detection of glomerular c-Abl mRNA and protein expression in different groups. *P < 0.05 versus control group at the same time point, #P < 0.05 versus Ang II infused group at the same time point. (E) and (F): Real-time PCR detection of c-Abl mRNA expression in cultured podocytes treated by Ang II at different doses and time points. (G) and (H): Western blot detection of c-Abl protein expression in cultured podocytes. *P < 0.05 versus control group or oh group.

Article Snippet: Embedded with osmotic mini-pump (Alzet model 2002 or 2004, CA), rats were randomly subjected to normal saline infusion, or Ang II infusion at 400 ng/kg/min, or Ang II at 400 ng/kg/min + STI-571 (Glivec, Novartis, Switzerland) at 50 mg/kg/day by means of intragastric administration for 14 or 28 days.

Techniques: Expressing, Cell Culture, Immunohistochemical staining, Staining, Negative Control, Real-time Polymerase Chain Reaction, Western Blot