BPR1K653 hydrochloride
BPR1K653 hydrochloride is a pan-Aurora kinase inhibitor, with an IC50 of 124.0 nM against Aurora-A and an IC50 of 45.0 nM against Aurora-B. BPR1K653 hydrochloride induces endoreduplication, apoptosis and antiproliferative activity in cancer cells. BPR1K653 hydrochloride can be used in research related to colon cancer and multidrug-resistant cancers.
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- CAS 番号: 1192754-07-6
- 分子式: C30H30Cl2N6O2
- 分子量:577.50
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Aurora Kinase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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Aurora A 124.0 nM (IC50) |
Aurora B 45.0 nM (IC50) |
体外実験
BPR1K653 hydrochloride is a pan-Aurora kinase inhibitor, with stronger inhibitory activity against purified Aurora-B kinase (IC50 = 45.0 nM) than against purified Aurora-A kinase (IC50 = 124.0 nM)[1].
BPR1K653 (0-10000 nM; administered 1 h after 24 h pretreatment with Nocodazole (HY-13520)) hydrochloride preferentially inhibits Aurora-B (Thr232) autophosphorylation over Aurora-A (Thr288) autophosphorylation in Nocodazole-arrested human colon cancer HCT116 cells, with IC50 values of 23.7 nM and 73.4 nM, respectively[1].
BPR1K653 hydrochloride potently inhibits the viability of human colon cancer cell line HCT116 (IC50 = 70 nM), and exhibits low toxicity toward normal human skin fibroblast cell line Detroit 551 (IC50 = 3.1 μM)[1].
BPR1K653 (10-1000 nM) hydrochloride inhibits aurora kinase activity in HCT116 colon cancer cells, as evidenced by concentration-dependent decreases in the levels of phosphorylated Aurora-A, Aurora-B, Aurora-C and phosphorylated histone H3[2].
BPR1K653 (third-generation culture cycle) hydrochloride potently inhibits the proliferation of various human cancer cell lines, regardless of tissue origin, p53 status, or the expression levels of MDR1 and MRP1 efflux pumps, with an IC50 value range of 4 nM to 135 nM[2].
BPR1K653 (10-20 h after thymidine release) hydrochloride significantly reduces the mitotic index of synchronized HeLa human cervical cancer cells[1].
BPR1K653 hydrochloride is a potent and selective pan-aurora kinase inhibitor, with an IC50 value of 124 nM against Aurora-A and 45 nM against Aurora-B, and exhibits extremely low activity against a panel of non-aurora kinases[2].
BPR1K653 (48 h) hydrochloride induces endoreplication and polyploidy in KB, MDR1-positive KB-VIN10 and HONE-1 human cancer cells in a concentration-dependent manner[2].
BPR1K653 (48 h) hydrochloride downregulates the expressions of phosphorylated histone H3 and cyclin B1 in a concentration-dependent manner in KB, MDR1-positive KB-VIN10 and HONE-1 human cancer cells[2].
BPR1K653 (48 h for Annexin-V, 60 h for caspase-3/-7 imaging, 72 h for TUNEL and PARP cleavage) hydrochloride induces apoptosis in human KB, MDR1-positive KB-VIN10, and HONE-1 cancer cells, which is confirmed by Annexin-V staining, caspase activation, DNA fragmentation, and PARP cleavage[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 human colon carcinoma cells
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Concentration:10-1000 nM
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Incubation Time:1 h (after 24 h Nocodazole pretreatment)
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Result:Inhibited autophosphorylation of Aurora-A (Thr288) with an IC50 of 73.4 nM.
Showed stronger inhibition of Aurora-B (Thr232) autophosphorylation with an IC50 of 23.7 nM.
Resulted in a cellular Aurora-A/B IC50 ratio of 3.1/1.
体内実験
BPR1K653 (15 mg/kg; i.p.; 5 days/week; 3 consecutive weeks) hydrochloride inhibits MDR1-positive KB-VIN10 cervical cancer xenograft growth by ~50% in nude mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice (male, 5-6 weeks old)[2]
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Dosage:15 mg/kg
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Administration:i.p.; 5 days/week; 2 consecutive weeks
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Result:Reduced the percentage of phosphor-Histone H3 positive tumor cells to 10% from controls.
Reduced tumor volume by ~73% compared to controls on day 30.
Induced 55% apoptotic cells in tumor tissue at 12 days post-treatment compared to controls.
Caused body weight loss of less than 10% relative to controls.
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Animal Model:Nude mice (male, 5-6 weeks old)[2]
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Dosage:15 mg/kg
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Administration:i.p.; 5 days/week; 3 consecutive weeks
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Result:Reduced tumor volume by ~50% compared to controls on day 42.
Caused body weight loss of less than 10% relative to controls.
化学情報
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CAS 番号 1192754-07-6
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分子量 577.50
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分子式 C30H30Cl2N6O2
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SMILES
O=C(NC1=CC=C(C=C1)CCNC2=C3C(OC(C4=CC=CC=C4)=C3Cl)=NC=N2)NC5=CC=CC=C5CN(C)C.Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BPR1K653 hydrochloride 関連分類
HY-120534 関連分類
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