4-[[(7R)-8-Cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide
BI 2536
CAS: 755038-02-9
Molecular Formula: C28H39N7O3
4-[[(7R)-8-Cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide - Names and Identifiers
4-[[(7R)-8-Cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide - Physico-chemical Properties
| Molecular Formula | C28H39N7O3 |
| Molar Mass | 521.65 |
| Density | 1.28 |
| Solubility | Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 25 mg/ml) |
| Appearance | Yellow powder. |
| Color | Off-white |
| pKa | 14.09±0.20(Predicted) |
| Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Use | BI 2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM, which is 4 and 11 times more selective than Plk2 and Plk3, respectively. |
| In vitro study | In addition to Plk1, BI 2536 also inhibited Plk2 and Plk3 activity, with only a low degree of inhibition, with an IC50 of 3.5 nM and 9.0 nM, respectively. BI 2536 was more than 1000-fold more selective than a group of 63 other protein kinases (IC50>10 μm). BI 2536 acts on HeLa cells at the dose of 10 nM to 100 nM, inhibits the recruitment of gamma-tubulin and Apc6 phosphorylation in mitotic centrosome, and inhibits the release of binding proteins in chromosome arms, induction of unipolar spindle, and some other plk1-dependent mitotic processes. Consistent with the effect of Plk1 RNAi, HeLa cells were treated with BI 2536 to stop the cell cycle at G2/M phase, followed by DNA breakdown and apoptosis, and the accumulation of fragmented PARP p85 fragments, this effect is concentration-dependent. BI 2536 inhibits the growth of a panel of 32 human tumor cell lines with EC50 of 2-25 nM, inhibits exponential growth by hTERT-RPE1, Human Umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cell proliferation, EC50 12-31 nM. BI 2536 inhibits Plk1, reduces the growth and viability of undifferentiated thyroid carcinoma (ATC) cells such as CAL62, OCUT-1, SW1736, 8505C, and ACT-1, the EC50 was 1.4-5.6 nM. |
| In vivo study | BI 2536 is administered intravenously to various xenograft tumor models, once or twice a week, with good results, inhibiting cell proliferation by arresting the cell cycle and subsequently inducing tumor cell death. BI 2536 at a dose of 50 mg/kg treated HCT 116 transplanted tumor, once or twice a week, significantly inhibited tumor growth, T/C was 15% and 0.3%, respectively. BI 2536 treated twice weekly in BxPC-3 and A549 models also significantly inhibited tumor growth with T/C of 5% and 14%, respectively. |
4-[[(7R)-8-Cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.917 ml | 9.585 ml | 19.17 ml |
| 5 mM | 0.383 ml | 1.917 ml | 3.834 ml |
| 10 mM | 0.192 ml | 0.958 ml | 1.917 ml |
| 5 mM | 0.038 ml | 0.192 ml | 0.383 ml |
Last Update：2024-01-02 23:10:35
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Featured ProductsSpot supply
Product Name: BI 2536 Visit Supplier Webpage Request for quotationCAS: 755038-02-9
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: BI 2536 Visit Supplier Webpage Request for quotationCAS: 755038-02-9
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: BI 2536 Visit Supplier Webpage Request for quotationCAS: 755038-02-9
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: BI 2536 Visit Supplier Webpage Request for quotationCAS: 755038-02-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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