产品
编 号：F006603
分子式：C15H18N6O
分子量：298.34
分子式：C15H18N6O
分子量：298.34
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规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 101622-51-9
产品详情
生物活性：
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM). Olomoucine regulates cell cycle and shows anti-melanin tumor activity.
体内研究：
Olomoucine (8 mg/kg; i.v.; once daily; 7 d) induces apoptosis in tumor cells on the 3rd day after treatment without side effects.Cassette dosing was found to overestimate the AUC while underestimating the Cmax compared with single dosing administration.Cassette dosing pharmacokinetics for olomoucine AdministrationCmax (nM)Clobs (l/h)Vss(obs) (l)MRTlast (h)AUCinf(obs) (nM.h)t1/2 (h)
cassettle9208 (0.9)1.100.67 (2.8)/td>0.5630301.03 (0.7)
single7194 (0.6)1.180.52 (2.1)/td>0.4028310.98 (0.7)
Note: Single agents dosing=50 mg/kg, cassette dosing=16.66 mg/kg.Animal Model:Dog with spontaneous melanoma (oral and maxillofacial tumors)
Dosage:8 mg/kg
Administration:Intravenous injection; once daily; for 7 days
Result:Induced programmed cell death of cancer cells and resulted in rapid eradication of at least 68% of the tumor cells.
Animal Model:Female Balb C? mice (6 weeks of age; weight of 20 g (±1.2 g))
Dosage:50 mg/kg (single agent) or 16.6 mg/kg combinded with purines (cassette)
Administration:Intravenous injection (tail vein); samples taken at 0.25, 0.5, 1, 2, 4, 6, and 24 h post-dosing
Result:Resulted faster plasma concentration decreasing with 50 mg/kg (as single agent) than 16.6 mg/kg (as cassette).
体外研究：
Olomoucine inhibits CDK2 and CDC2 kinases with IC50 of 7 μM (CDC2/cyclin B), 7 μM (CDK2/cyclin A), 7 μM (CDK2/cyclin E), 3 Μm (CDK5/p35), and 25μM (ERK1/p44 MAPK), respectively.Olomoucine (0, 5, 10, 15, and 25 μM) is a competitive inhibitor for ATP and as a non-competitive inhibitor for histone H.Olomoucine (0-1000 μM) inhibits DNA synthesis in interleukin-2-stimulated T lymphocytes (CTLL-2 cells) and triggers a Gl arrest similar to interleukin-2 deprivation.Olomoucine (0-100 μM) inhibits Gl/S transition of non-small cell lung cancer cell line MB65 cells.Olomoucine (0-150 μM) inhibits prophase/metaphase transition of Rdditapes oocytes.Olomoucine inhibits tumor cells survival with IC50s of 32.35 μM (dog melanoma), 42.15 μM (mouse B16 melanoma), 82.30 μM (human melanoma), respectively.
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM). Olomoucine regulates cell cycle and shows anti-melanin tumor activity.
体内研究：
Olomoucine (8 mg/kg; i.v.; once daily; 7 d) induces apoptosis in tumor cells on the 3rd day after treatment without side effects.Cassette dosing was found to overestimate the AUC while underestimating the Cmax compared with single dosing administration.Cassette dosing pharmacokinetics for olomoucine AdministrationCmax (nM)Clobs (l/h)Vss(obs) (l)MRTlast (h)AUCinf(obs) (nM.h)t1/2 (h)
cassettle9208 (0.9)1.100.67 (2.8)/td>0.5630301.03 (0.7)
single7194 (0.6)1.180.52 (2.1)/td>0.4028310.98 (0.7)
Note: Single agents dosing=50 mg/kg, cassette dosing=16.66 mg/kg.Animal Model:Dog with spontaneous melanoma (oral and maxillofacial tumors)
Dosage:8 mg/kg
Administration:Intravenous injection; once daily; for 7 days
Result:Induced programmed cell death of cancer cells and resulted in rapid eradication of at least 68% of the tumor cells.
Animal Model:Female Balb C? mice (6 weeks of age; weight of 20 g (±1.2 g))
Dosage:50 mg/kg (single agent) or 16.6 mg/kg combinded with purines (cassette)
Administration:Intravenous injection (tail vein); samples taken at 0.25, 0.5, 1, 2, 4, 6, and 24 h post-dosing
Result:Resulted faster plasma concentration decreasing with 50 mg/kg (as single agent) than 16.6 mg/kg (as cassette).
体外研究：
Olomoucine inhibits CDK2 and CDC2 kinases with IC50 of 7 μM (CDC2/cyclin B), 7 μM (CDK2/cyclin A), 7 μM (CDK2/cyclin E), 3 Μm (CDK5/p35), and 25μM (ERK1/p44 MAPK), respectively.Olomoucine (0, 5, 10, 15, and 25 μM) is a competitive inhibitor for ATP and as a non-competitive inhibitor for histone H.Olomoucine (0-1000 μM) inhibits DNA synthesis in interleukin-2-stimulated T lymphocytes (CTLL-2 cells) and triggers a Gl arrest similar to interleukin-2 deprivation.Olomoucine (0-100 μM) inhibits Gl/S transition of non-small cell lung cancer cell line MB65 cells.Olomoucine (0-150 μM) inhibits prophase/metaphase transition of Rdditapes oocytes.Olomoucine inhibits tumor cells survival with IC50s of 32.35 μM (dog melanoma), 42.15 μM (mouse B16 melanoma), 82.30 μM (human melanoma), respectively.
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