产品
编 号：F610355
分子式：C24H22N2O
分子量：354.44
分子式：C24H22N2O
分子量：354.44
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 883561-04-4
产品详情
生物活性：
CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 μM. CA224 induces cell apoptosis and shows antitumor activity.
体内研究：
CA224 (Compound 1) (100 mg/kg; i.p.; once a day for 9 days) shows significant tumor growth inhibition without obvious toxicity.Animal Model:The severe combined immunodeficient (SCID) mouse, lacking both T and B immune cells. Male mice weighing 18?25 g, 6?8 weeks of age for subcutaneous injection of HCT-116, female mice weighing 15?24 g, 6?8 weeks of age for subcutaneous injection of NCI-H460
Dosage:100 mg/kg
Administration:Intraperitoneal injection, once a day for 9 consecutive days
Result:Showed significant tumor growth inhibition in both HCT-116 and NCI-H460 tumor models without significant bodyweight loss.
Animal Model:BALB/c mice
Dosage:10 mg/kg (oral administration) or 1.0 mg/kg (intravenous injection)
Administration:Oral or intravenous injection (Pharmacokinetics Analysis)
Result:Pharmacokinetics parameters determined for CA224 after IV and PO administration.ParameterIV (1 mg/kg) Oral (10 mg/kg)
t1/2,β (h)0.331.16
AUC0-t (ng·h/mL)187172
AUC0-∞ (ng·h/mL)189182
Cmax (ng/mL)371190
Vd (L/Kg)2.52nd
Vdss (L/Kg)1.76nd
CL (mL/min/kg)88.3nd
Bioavailability-9.6%
Time points consideredfor t1/2,β calculation0.5-2 h1-4 h
体外研究：
CA224 (Compound 1) (48 h) shows antiproliferation activity against human cancer cell lines.CA224 (18-48 h) blocks the growth of cancer cells at G0/G1 and G2/M phase of the cell cycle, and selectively kills SV40 large T-antigen transformed normal mouse embryonic liver cells (BNL SV A.8).CA224 (0-4 μM, 30 min) inhibits tubulin polymerization and enhances the depolymerization of stabilized tubulin protein.CA224 (0-72 h) induces cell apoptosis in cancer cells.CA224 (10 μM) shows 50%, 14%, 51% and 19% inhibition of CYP3A4, CYP2D6, CYP2C9, and CYP2C19, respectively.
CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 μM. CA224 induces cell apoptosis and shows antitumor activity.
体内研究：
CA224 (Compound 1) (100 mg/kg; i.p.; once a day for 9 days) shows significant tumor growth inhibition without obvious toxicity.Animal Model:The severe combined immunodeficient (SCID) mouse, lacking both T and B immune cells. Male mice weighing 18?25 g, 6?8 weeks of age for subcutaneous injection of HCT-116, female mice weighing 15?24 g, 6?8 weeks of age for subcutaneous injection of NCI-H460
Dosage:100 mg/kg
Administration:Intraperitoneal injection, once a day for 9 consecutive days
Result:Showed significant tumor growth inhibition in both HCT-116 and NCI-H460 tumor models without significant bodyweight loss.
Animal Model:BALB/c mice
Dosage:10 mg/kg (oral administration) or 1.0 mg/kg (intravenous injection)
Administration:Oral or intravenous injection (Pharmacokinetics Analysis)
Result:Pharmacokinetics parameters determined for CA224 after IV and PO administration.ParameterIV (1 mg/kg) Oral (10 mg/kg)
t1/2,β (h)0.331.16
AUC0-t (ng·h/mL)187172
AUC0-∞ (ng·h/mL)189182
Cmax (ng/mL)371190
Vd (L/Kg)2.52nd
Vdss (L/Kg)1.76nd
CL (mL/min/kg)88.3nd
Bioavailability-9.6%
Time points consideredfor t1/2,β calculation0.5-2 h1-4 h
体外研究：
CA224 (Compound 1) (48 h) shows antiproliferation activity against human cancer cell lines.CA224 (18-48 h) blocks the growth of cancer cells at G0/G1 and G2/M phase of the cell cycle, and selectively kills SV40 large T-antigen transformed normal mouse embryonic liver cells (BNL SV A.8).CA224 (0-4 μM, 30 min) inhibits tubulin polymerization and enhances the depolymerization of stabilized tubulin protein.CA224 (0-72 h) induces cell apoptosis in cancer cells.CA224 (10 μM) shows 50%, 14%, 51% and 19% inhibition of CYP3A4, CYP2D6, CYP2C9, and CYP2C19, respectively.
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