Benzamide, N-(3-aminopropyl)-N-((1R)-1-(7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl)-2-methylpropyl)-4-methyl-
Ispinesib (SB-715992)
CAS: 336113-53-2
Molecular Formula: C30H33ClN4O2
Benzamide, N-(3-aminopropyl)-N-((1R)-1-(7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl)-2-methylpropyl)-4-methyl- - Names and Identifiers
Benzamide, N-(3-aminopropyl)-N-((1R)-1-(7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl)-2-methylpropyl)-4-methyl- - Physico-chemical Properties
| Molecular Formula | C30H33ClN4O2 |
| Molar Mass | 517.06 |
| Density | 1.21±0.1 g/cm3(Predicted) |
| Melting Point | 89 - 92°C |
| Boling Point | 708.0±70.0 °C(Predicted) |
| Solubility | Chloroform (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 9.65±0.10(Predicted) |
| Storage Condition | -20°C Freezer, Under inert atmosphere |
| In vitro study | Ispinesib is a potent reversible allosteric inhibitor of specific KSP, and the binding property of KSP to microtubules perturbs the movement of KSP by inhibiting the release of ADP without changing the release of KSP-ADP complexes in microtubules. Ispinesib acts on a range of tumor cell lines, including Colo205, Colo201, HT-29, M5076, Madison-109, and MX-1, with an IC50 of 1.2 nM to 9.5 nM and is highly cytotoxic. 15 nM and 30 nM Ispinesib act on PC-3 prostate cancer cells by regulating expression levels of genes that control apoptosis, cell proliferation, cell cycle, and signaling, such as EGFR, p27, p15, and IL-11, inhibit cell proliferation and induce apoptosis. 7.4 nM-600 nM Ispinesib has broad-spectrum inhibitory activity against a panel of 53 breast cancer cell lines. 150 nM Ispinesib acts on BT-474 and MDA-MB-468 cells, induces apoptosis, increases the proportion of apoptotic cells, decreases the level of anti-apoptotic Bcl-XL, and increases the levels of pro-apoptotic Bax and Bid. |
| In vivo study | Ispinesib at a dose of 4.5 mg/kg-15 mg/kg in a mouse model bearing transplanted tumors effectively inhibited Colo205, Colo201, and HT-29 cells, but did not inhibit MX-1 cells. SB-715992 treatment at doses ranging from 6 mg/kg to 10 mg/kg also inhibited solid tumors in mice, including Madison 109 lung carcinoma, M5076 sarcoma, and L1210 and P388 leukemias. Ispinesib inhibits tumor growth in mice bearing xenografts of breast cancer cells MCF-7, HCC1954, MDA-MB-468, and KPL4 at doses of 8 mg/kg to 10 mg/kg. |
Benzamide, N-(3-aminopropyl)-N-((1R)-1-(7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl)-2-methylpropyl)-4-methyl- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.934 ml | 9.67 ml | 19.34 ml |
| 5 mM | 0.387 ml | 1.934 ml | 3.868 ml |
| 10 mM | 0.193 ml | 0.967 ml | 1.934 ml |
| 5 mM | 0.039 ml | 0.193 ml | 0.387 ml |
Last Update：2024-01-02 23:10:35
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Product Name: Ispinesib Visit Supplier Webpage Request for quotationCAS: 336113-53-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: Ispinesib (SB-715992) Visit Supplier Webpage Request for quotation
CAS: 336113-53-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 336113-53-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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