MLN8054
MLN8054
CAS: 869363-13-3
Molecular Formula: C25H15ClF2N4O2
MLN8054 - Names and Identifiers
MLN8054 - Physico-chemical Properties
| Molecular Formula | C25H15ClF2N4O2 |
| Molar Mass | 476.86 |
| Density | 1.48 |
| Boling Point | 694.9±65.0 °C(Predicted) |
| pKa | 4.18±0.10(Predicted) |
| Storage Condition | -20℃ |
| Use | MLN8054 is a highly effective, selective, orally active aurora kinase (aurora A) inhibitor with an IC50 value of 4 nM. |
| In vitro study | MLN8054 is A reversible inhibitor of ATP-competitive recombinant Aurora A kinase with an IC50 of 4 nM and is more than 40-fold more selective for inhibition of Aurora A than for inhibition of Aurora B. In vitro, MLN8054 can inhibit the growth of various tissue and organ cell lines with IC50 of 0.11 μm to 1.43 μm. In addition, MLN8054 acts on cultured cells, selectively inhibits Aurora A but not Aurora B, and acts on A variety of cultured human tumor cell lines to inhibit cell proliferation by promoting G2/M accumulation and spindle derangement. Recent studies have shown that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with persistent DNA double-strand breaks. MLN8054 is A reversible inhibitor of ATP-competitive recombinant Aurora A kinase with an IC50 of 4 nM, and is more than 40-fold more selective for inhibition of Aurora A than for inhibition of Aurora B. In vitro, MLN8054 can inhibit the growth of various tissue and organ cell lines with IC50 of 0.11 μm to 1.43 μm. In addition, MLN8054 acts on cultured cells, selectively inhibits Aurora A but not Aurora B, and acts on A variety of cultured human tumor cell lines to inhibit cell proliferation by promoting G2/M accumulation and spindle derangement. Recent studies have shown that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with persistent DNA double-strand breaks. |
| In vivo study | MLN8054 was orally administered to mice with HCT-116 tumors at doses of 3 mg/kg, 10 mg/kg, and 30 mg/kg once a day, the 10 mg/kg and 30 mg/kg dose treatments resulted in 76% and 84% inhibition of tumor growth, respectively, in a dose-dependent manner. MLN8054 has similar anticancer activity in nude mice with PC-3 transplanted tumor. MLN8054 was used to induce DNA and microtubule staining of tumor tissue in the nucleus and cell region in the animal model carrying HCT-116 transplanted tumor, which is consistent with the aging performance, by increasing aging-associated beta-galactosidase activity MLN8054 mice bearing HCT-116 tumors were orally dosed at 3 mg/kg, 10 mg/kg, and 30 mg/kg, treatment at doses of 10 mg/kg and 30 mg/kg once daily resulted in tumor growth inhibition of 76% and 84%, respectively, in a dose-dependent manner. MLN8054 has similar anticancer activity in nude mice with PC-3 transplanted tumor. MLN8054 acts on the animal model carrying HCT-116 transplanted tumor to induce DNA and microtubule staining of tumor tissue in the nucleus and cell region, which is consistent with the expression of aging. By increasing the activity of beta-galactosidase associated with aging |
MLN8054 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.097 ml | 10.485 ml | 20.971 ml |
| 5 mM | 0.419 ml | 2.097 ml | 4.194 ml |
| 10 mM | 0.21 ml | 1.049 ml | 2.097 ml |
| 5 mM | 0.042 ml | 0.21 ml | 0.419 ml |
Last Update：2024-01-02 23:10:35
MLN8054 - Reference Information
| biological activity | MLN8054 is an effective and selective Aurora A inhibitor with IC50 of 4 nM, which is 40 times more selective on Aurora A than on Aurora B. Phase 1. MLN8054 is an effective, selective Aurora A inhibitor. The IC50 in Sf9 insect cells is 4 nM, and the selectivity for Aurora A is 40 times higher than that for Aurora B. Phase 1. |
| in vitro study | MLN8054 is a reversible inhibitor of ATP competitive recombinant Aurora A kinase with IC50 of 4 nM. The selectivity of inhibiting Aurora A is more than 40 times higher than that of inhibiting Aurora B. In vitro, MLN8054 can inhibit the growth of various tissue and organ cell lines with IC50 ranging from 0.11 μM to 1.43 μM. In addition, MLN8054 acts on cultured cells to selectively inhibit Aurora A instead of Aurora B, and acts on various cultured human tumor cell lines to inhibit cell proliferation by promoting G2/M accumulation and spindle disorder. Recent research shows that MLN8054 sensitize androgen-resistant prostate cancer to radioactivity by inhibiting Aurora A kinase, which is related to persistent DNA double-strand breaks. MLN8054 is a reversible inhibitor of ATP competitive recombinant Aurora A kinase with IC50 of 4 nM. The selectivity of inhibiting Aurora A is more than 40 times higher than that of inhibiting Aurora B. In vitro, MLN8054 can inhibit the growth of various tissue and organ cell lines with IC50 ranging from 0.11 μM to 1.43 μM. In addition, MLN8054 acts on cultured cells to selectively inhibit Aurora A instead of Aurora B, and acts on various cultured human tumor cell lines to inhibit cell proliferation by promoting G2/M accumulation and spindle disorder. Recent research shows that MLN8054 sensitize androgen-resistant prostate cancer to radioactivity by inhibiting Aurora A kinase, which is related to persistent DNA double-strand breaks. |
| in vivo study | MLN8054 is orally administered to mice carrying HCT-116 tumors at doses of 3 mg/kg, 10 mg/kg, and 30 mg/kg. once a day, 10 mg/kg and 30 mg/kg dose treatment results in tumor growth inhibition of 76% and 84% respectively. this effect is dose-dependent. MLN8054 acts on nude mice carrying PC-3 transplanted tumors and has similar anticancer activity. MLN8054 acts on the animal model carrying HCT-116 transplanted tumor, induces DNA and microtubule staining of tumor tissue in the nucleus and cell body region, which is consistent with the performance of aging. by improving the aging-related beta-galactosidase activity MLN8054, mice carrying HCT-116 tumor are orally administered at doses of 3 mg/kg, 10 mg/kg, and 30 mg/kg, once a day, 10 mg/kg and 30 mg/kg dose treatment resulted in tumor growth inhibition of 76% and 84%, respectively, which was dose-dependent. MLN8054 acts on nude mice carrying PC-3 transplanted tumors and has similar anticancer activity. MLN8054 acts on animal models carrying HCT-116 transplanted tumors to induce DNA and microtubule staining of tumor tissues in the nucleus and cell body regions, which is consistent with the performance of aging. by improving the aging-related beta-galactosidase activity |
| features | MLN8054 are effective selective inhibitors of Aurora A kinase. |
| target | TargetValue Aurora A (Sf9 cells) 4 nM Aurora B (Sf9 cells) 172 nM |
| Target | Value |
| Aurora A (Sf9 cells) | 4 nM |
| Aurora B (Sf9 cells) | 172 nM |
Last Update：2024-04-09 20:49:11
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Spot supply
Product Name: MLN8054 Visit Supplier Webpage Request for quotationCAS: 869363-13-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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