2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. Contragestazol

Contragestazol (DL111-IT) 是一种非激素类抗生育剂。Contragestazol 可降低 Cyclin D1 和 CDK4 的表达，增加总视网膜母细胞瘤蛋白 (pRb) 的表达，并降低过度磷酸化的 pRb 水平。Contragestazol 可诱导 G0/G1 期细胞周期阻滞。Contragestazol 通过诱导黄体细胞凋亡 (Apoptosis) 及降低子宫内多胺水平，从而抑制胚胎发育。Contragestazol 对前列腺癌、 S180 肿瘤和 H22 肿瘤具有抗肿瘤活性。Contragestazol 在动物体内表现出极强的终止早期妊娠活性。

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Contragestazol

Contragestazol Chemical Structure

CAS No. : 69095-83-6

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Contragestazol 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Contragestazol (DL111-IT) is a non-hormonal antifertility agent. Contragestazol reduces the expression of Cyclin D1 and CDK4, increases the expression of total retinoblastoma protein (pRb), and decreases the level of hyperphosphorylated pRb. Contragestazol induces G0/G1 phase cell cycle arrest. Contragestazol inhibits embryonic development by inducing luteal cell apoptosis and reducing intrauterine polyamine levels. Contragestazol exhibits antitumor activity against prostate cancer, S180 tumor and H22 tumor. Contragestazol shows extremely potent activity in terminating early pregnancy in animals[1][2].

IC50 & Target[1]

CDK4

 

体外研究
(In Vitro)

Contragestazol (2.5-40 μg/mL; 48 h) 可在作用 48 小时后以剂量依赖方式抑制 12 种受试癌细胞系 (包括 P388、HO-8910 和 A549) 的增殖，其 IC50 值范围为 4.1 至 17.4 μg/mL[1]。
Contragestazol (1.5-6.0 μg/mL; 24-144 h) 呈时间依赖性抑制 HO-8910 卵巢癌细胞的增殖[1]。
Contragestazol (5.0-20.0 μg/mL; 48 h) 可在暴露 48 小时后诱导 HO-8910 卵巢癌细胞发生剂量依赖性 G0/G1 期细胞周期阻滞[1]。
Contragestazol (5.0-20.0 μg/mL; 24 h) 可在人 HO-8910 卵巢癌细胞暴露 24 h 后调控细胞周期调控蛋白的表达，以剂量依赖方式增加总 pRb 水平、降低高磷酸化 pRb 水平，并下调 Cyclin D1 和 CDK4 的表达[1]。
Contragestazol (DL111-IT) (2.5-40 µg/mL; 48 h) 可在体外强效抑制雄激素非依赖性前列腺癌细胞系 PC3 的增殖，其 IC50 为 9.9 µg/mL[2]。
Contragestazol (DL111-IT) (5-20 µg/mL; 48 h) 可在雄激素非依赖性前列腺癌细胞系 PC3 中诱导剂量依赖性的 G0/G1 期细胞周期阻滞 (无细胞凋亡)[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Contragestazol 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HO-8910, KB, HCT116, K562, CNE, RD, A549, Hela, HL60, PC3, Bel7402, P388
Concentration: 2.5 μg/mL, 5 μg/mL, 10 μg/mL, 20 μg/mL, 40 μg/mL
Incubation Time: 48 h
Result: Induced dose-dependent sensitivity in all 12 tested cell lines.
Resulted in IC50 values ranging from 4.1 μg/mL (P388 cells) to 17.4 μg/mL (A549 cells).

Cell Proliferation Assay[1]

Cell Line: HO-8910
Concentration: 1.5 μg/mL, 6.0 μg/mL
Incubation Time: 24-144 h
Result: Exerted mild cytotoxicity at 1.5 μg/mL and stronger cell killing activity in a time-dependent manner at 6.0 μg/mL.
Achieved proliferation inhibition rates of 20.5% (P<0.05) at 1.5 μg/mL and 41.0% (P<0.01) at 6.0 μg/mL after 144 h.

Cell Cycle Analysis[1]

Cell Line: HO-8910
Concentration: 5.0 μg/mL, 10.0 μg/mL, 20.0 μg/mL
Incubation Time: 48 h
Result: Induced dose-dependent G0/G1 cell cycle arrest in HO-8910 cells.
Increased the percentage of cells in G0/G1 phase to 43.8% at 5.0 μg/mL, 66.2% at 10.0 μg/mL, and 76.2% at 20.0 μg/mL.
Decreased the proportion of cells in S phase in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: HO-8910
Concentration: 5.0 μg/mL, 10.0 μg/mL, 20.0 μg/mL
Incubation Time: 24 h
Result: Increased total pRb protein levels in a dose-dependent manner.
Decreased hyperphosphorylated pRb levels in a dose-dependent manner.
Reduced Cyclin D1 and CDK4 protein expression at 10.0 and 20.0 μg/mL in a dose-dependent pattern.

Cell Proliferation Assay[2]

Cell Line: human androgen-independent prostate cancer cell line PC3
Concentration: 2.5 µg/mL, 5.00 µg/mL, 10.00 µg/mL, 20.00 µg/mL, 40.00 µg/mL
Incubation Time: 48 h
Result: Dose-dependently inhibited PC3 cell proliferation.
Achieved an IC50 value of 9.9 µg/mL.
体内研究
(In Vivo)

Contragestazol (DL111-IT) (12.5-50.0 mg/kg；肌肉注射；每日 1 次；连续 9 天) 可剂量依赖性地抑制雄性 ICR 小鼠的 S180 肿瘤生长，其中 50.0 mg/kg 剂量的肿瘤抑制率达 55.9%[1]。
Contragestazol (DL111-IT) (12.5-50.0 mg/kg；肌肉注射；每日 1 次；连续 9 天) 可剂量依赖性地抑制雄性 ICR 小鼠体内 H22 肿瘤的生长，其中 50.0 mg/kg 剂量的肿瘤抑制率达 56.6%[1]。
Contragestazol (DL111-IT) (12.5-50.0 mg/kg；肌肉注射；每周 4 次；共 15 天) 可剂量依赖性地抑制雌性 Balb/c 裸鼠体内 HO-8910 异种移植瘤的生长，其中 50.0 mg/kg 剂量组的肿瘤重量抑制率达 64.8%[1]。
Contragestazol (DL111-IT) (1.25-20.0 mg/kg；肌肉注射；每日 1 次；连续 10 天) 可剂量依赖性地抑制 Balb/c 雌性无胸腺裸鼠体内 PC3 前列腺癌异种移植物的生长，在 1.25 mg/kg 至 20.0 mg/kg 剂量下的肿瘤重量抑制率为 20.8% 至 50.0%，且不影响小鼠体重[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR (male)[1]
Dosage: 12.5 mg/kg; 25.0 mg/kg; 50.0 mg/kg
Administration: i.m.; once daily; 9 consecutive days
Result: Achieved a 33.6% tumor inhibition rate (S180).
Achieved a 50.0% tumor inhibition rate (S180).
Achieved a 55.9% tumor inhibition rate (S180).\n
Achieved a 24.5% tumor inhibition rate (H22).
Achieved a 52.0% tumor inhibition rate (H22).
Achieved a 56.6% tumor inhibition rate (H22).
Animal Model: Balb/c athymic nude (female, 4- to 5-week-old)[1]
Dosage: 12.5 mg/kg; 25.0 mg/kg; 50.0 mg/kg
Administration: i.m.; four times per week; 15 days
Result: Achieved a 17.1% tumor weight inhibition rate (no statistical significance reported) and a 7.7-fold increase in tumor volume from baseline.
Achieved a 44.8% tumor weight inhibition rate (P<0.001), significant tumor volume inhibition starting at day 7 (P<0.01-0.001), and a 5.3-fold increase in tumor volume from baseline.
Achieved a 64.8% tumor weight inhibition rate (P<0.001), significant tumor volume inhibition starting at day 7 (P<0.01-0.001), and a 3.9-fold increase in tumor volume from baseline.
Caused no significant effect on mouse body weight for any dose.
Animal Model: Balb/c (female, athymic nude, 4- to 5-week-old, subcutaneous injection of PC3 human prostate cancer cells)[2]
Dosage: 1.25 mg/kg; 5.0 mg/kg; 20.0 mg/kg
Administration: i.m.; once daily; 10 days
Result: Inhibited tumor volumes significantly (P < 0.05-0.01) in the 5.0 mg/kg and 20.0 mg/kg groups at day 4.
Reduced tumor growth rate (P < 0.05) in the 1.25 mg/kg group starting at day 6.
Increased tumor volumes 3.5-fold, 2.6-fold, and 2.0-fold in the 1.25 mg/kg, 5.0 mg/kg, and 20.0 mg/kg groups respectively by day 13, compared to 6.7-fold in control group.
Achieved tumor weight inhibition rates of 20.8% (1.25 mg/kg), 41.7% (5.0 mg/kg), and 50.0% (20.0 mg/kg).
Caused no significant changes in animal body weight across treatment groups.
分子量

279.34

Formula

C17H17N3O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Contragestazol 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Contragestazol69095-83-6DL111-ITCDKApoptosisCyclin dependent kinaseA549androgen-independent prostate cancerCDK4P388Cyclin D1HO-8910retinoblastoma proteincorpus luteumprogesterone3β-hydroxysteroid dehydrogenaseInhibitorinhibitorinhibit

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