TC-S 7010 (Aurora A Inhibitor I)
Aurora A Inhibitor I
CAS: 1158838-45-9
Molecular Formula: C31H31ClFN7O2
TC-S 7010 (Aurora A Inhibitor I) - Names and Identifiers
TC-S 7010 (Aurora A Inhibitor I) - Physico-chemical Properties
| Molecular Formula | C31H31ClFN7O2 |
| Molar Mass | 588.07 |
| Density | 1.362 |
| Solubility | DMSO: soluble10mg/mL, clear |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | 2-8°C |
| In vitro study | Aurora A Inhibitor I is 1000 times more selective for Aurora A than for Aurora B. However, Aurora A Inhibitor I has little effect on Aurora A (T217E), which is A mutant Aurora A in which A single amino acid is replaced. Thr217 of Aurora A is A key amino acid residue that binds to the inhibitor and determines that the selectivity is higher than that of Aurora B. Aurora A Inhibitor I effectively inhibited HCT116 proliferation with an IC50 of 0.19 μm, The effect on HCT29 was not significant, with IC50 of 2.9 μm. The latest study showed that Aurora A Inhibitor I accumulated KCL-22 cells in G2/M, but did not induce polyploidy. Aurora A Inhibitor I induces phosphorylation of histone H3 at serine 10 and inhibits mitotic Aurora A autophosphorylation at threonine 288. 5 M Aurora A Inhibitor I significantly induced KCL-22 cell apoptosis, and the cells were sensitive to imatinib induced apoptosis. Aurora A Inhibitor I also inhibited the growth of KG-1 and HL-60 cells, but did not sensitize the cells to imatinib-induced apoptosis. Aurora A Inhibitor I also inhibits the normal cell line wi38. 1 μm Aurora A Inhibitor I blocked BCR-ABL mutation formation, KCL-22 relapse after treatment with imatinib, nilotinib or dasatinib, and Mutant colonies. Aurora A Inhibitor I is 1000 times more selective for Aurora A than for Aurora B. But the effect of Aurora A Inhibitor I on Aurora A (T217E) (T217E) is A mutant Aurora A with A single amino acid substitution. Thr217 of Aurora A is A key amino acid residue that binds to the inhibitor and determines that the selectivity is higher than that of Aurora B. Aurora A Inhibitor I effectively inhibited HCT116 proliferation with an IC50 of 0.19 μm, but had little effect on HCT29 with an IC50 of 2.9 μm. Recent studies have shown that Aurora A Inhibitor I allows KCL-22 cells to accumulate at G2/M, but does not induce polyploidy. Aurora A Inhibitor I induces phosphorylation of histone H3 at serine 10 and inhibits mitotic Aurora A autophosphorylation at threonine 288. 5 M Aurora A Inhibitor I significantly induced KCL-22 cell apoptosis, and the cells were sensitive to imatinib induced apoptosis. Aurora A Inhibitor I also inhibited the growth of KG-1 and HL-60 cells, but did not sensitize the cells to imatinib-induced apoptosis. Aurora A Inhibitor I also inhibits the normal cell line wi38. 1 μm Aurora A Inhibitor I blocked BCR-ABL mutation formation, KCL-22 relapse after treatment with imatinib, nilotinib or dasatinib, and Mutant colonies. |
TC-S 7010 (Aurora A Inhibitor I) - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| WGK Germany | 3 |
TC-S 7010 (Aurora A Inhibitor I) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.7 ml | 8.502 ml | 17.005 ml |
| 5 mM | 0.34 ml | 1.7 ml | 3.401 ml |
| 10 mM | 0.17 ml | 0.85 ml | 1.7 ml |
| 5 mM | 0.034 ml | 0.17 ml | 0.34 ml |
Last Update：2024-01-02 23:10:35
TC-S 7010 (Aurora A Inhibitor I) - Reference Information
| biological activity | Aurora A Inhibitor I is a new effective and selective Aurora A inhibitor with IC50 of 3.4 nM, which is 1000 times more selective than Aurora B. Aurora A Inhibitor I (TC-S 7010) is a new effective and selective Aurora A inhibitor. IC50 is 3.4 nM in cell-free test, and the selectivity for Aurora A is 1000 times higher than that for Aurora B. Aurora A Inhibitor I (TC-S 7010) can trigger apoptosis through ROS-mediated UPR signaling pathway. |
| in vitro study | Aurora A Inhibitor I is 1000 times more selective than Aurora B. However, Aurora A Inhibitor I has little effect on Aurora A (T217E). Aurora A (T217E) is a mutant Aurora A with a single amino acid replaced. Aurora A's Thr217 is a key amino acid residue that binds to the inhibitor and determines a higher selectivity than Aurora B. Aurora A Inhibitor I effectively inhibited the proliferation of HCT116, IC50 was 0.19 μM, but had little effect on HCT29, IC50 was 2.9 μM. The latest research showed that Aurora A Inhibitor I made KCL-22 cells accumulate in G2/M, but did not induce polyploidy. Aurora A Inhibitor I induces phosphorylation of histone H3 at serine 10 site and inhibits autophosphorylation of mitotic Aurora A at threonine 288 site. 5 μM Aurora A Inhibitor I obviously induced apoptosis of KCL-22 cells and made cells sensitive to imatinib-induced apoptosis. Aurora A Inhibitor I also inhibited the growth of KG-1 and HL-60 cells, but did not sensitize the cells to imatinib-induced apoptosis. Aurora A Inhibitor I also inhibited the normal cell line WI38. 1 μM Aurora A Inhibitor I blocks the formation of BCR-ABL mutations, KCL-22 recurrence after imatinib, nilotinib or dasatinib treatment, and mutant colonies. Aurora A Inhibitor I is 1000 times more selective than Aurora B. However, Aurora A Inhibitor I has little effect on Aurora A (T217E). Aurora A (T217E) is a mutant Aurora A with a single amino acid replaced. Aurora A's Thr217 is a key amino acid residue that binds to the inhibitor and determines a higher selectivity than Aurora B. Aurora A Inhibitor I effectively inhibited the proliferation of HCT116, IC50 was 0.19 μM, but had little effect on HCT29, IC50 was 2.9 μM. The latest research showed that Aurora A Inhibitor I made KCL-22 cells accumulate in G2/M, but did not induce polyploidy. Aurora A Inhibitor I induces phosphorylation of histone H3 at serine 10 site and inhibits autophosphorylation of mitotic Aurora A at threonine 288 site. 5 μM Aurora A Inhibitor I obviously induced apoptosis of KCL-22 cells and made cells sensitive to imatinib-induced apoptosis. Aurora A Inhibitor I also inhibited the growth of KG-1 and HL-60 cells, but did not sensitize the cells to imatinib-induced apoptosis. Aurora A Inhibitor I also inhibited the normal cell line WI38. 1 μM Aurora A Inhibitor I blocks the formation of BCR-ABL mutations, KCL-22 recurrence after imatinib, nilotinib or dasatinib treatment, and mutant colonies. |
| characteristics | AuroraA Inhibitor I is a 2, 4-diphenylamine pyrimidine inhibitor. |
| target | TargetValue Aurora A (Cell-free say) 3.4 nM |
| Target | Value |
| Aurora A (Cell-free assay) | 3.4 nM |
Last Update：2024-04-09 21:31:57
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Product Name: Aurora A Inhibitor I Visit Supplier Webpage Request for quotationCAS: 1158838-45-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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