Dinaciclib (Synonyms:SCH 727965)
目录号 : KM2617 CAS No. : 779353-01-4 纯度 : 98%

Dinaciclib (SCH 727965) 是一种有效的选择性 CDK 抑制剂,抑制 CDK2,CDK5,CDK1 和 CDK9 的 IC50 分别为 1 nM,1 nM,3 nM 和 4 nM。

规格 价格 是否有货 数量
5mg
In-stock
10mg
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50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC50s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively.

体外研究

Dinaciclib (SCH 727965) is a potent DNA replication inhibitor that blocks thymidine (dThd) DNA incorporation in A2780 cells with an IC50 of 4 nM. Dinaciclib (100 nM) inhibits phosphorylation of the retinoblastoma (Rb) tumor suppressor protein and induces accumulation of the p85 PARP caspase cleavage product. In vitro cell growth of pancreatic cancer cells is inhibited by Dinaciclib (SCH727965) in a dose-dependent manner. Upon incubation with Dinaciclib for 72 h, the GI50s are approximately 10 and 20 nM for MIAPaCa-2 and Pa20C cells, respectively. These results are consistent with studies of Dinaciclib in other cancer cell lines. In soft agar assays, 5 to 10 nM of Dinaciclib significantly reduces colony formation and anchorage independent growth of MIAPaCa-2 cells. Moreover, in vitro cell migration of Pa20C and MIAPaCa-2 cells is significantly reduced by Dinaciclib-concentrations starting from 2-5 nM, as demonstrated using BD FluoroChrom, modified Boyden Chamber and wound healing assays.

体内研究

Dinaciclib (8, 16, 32, and 48 mg/kg, i.p.) results in tumor inhibition by 70%, 70%, 89%, and 96%, respectively; Dinaciclib (SCH 727965) is well tolerated, and the maximum body weight loss in the highest dosage group is 5%. Dinaciclib has a short plasma half-life in mouse. A dose of 5 mg/kg Dinaciclib given i.p. in mice is associated with a plasma half-life of ~0.25 hour. Treatment with Dinaciclib (SCH727965) given as twice weekly i.p. doses of 40 mg/kg for 4 weeks causes significant tumor growth inhibition (TGI) in 10/10 (100%) of low-passage subcutaneous pancreatic xenografts tested.

分子式
C21H28N6O2
分子量
396.49
CAS号
779353-01-4
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (252.21 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5221 mL 12.6107 mL 25.2213 mL
5 mM 0.5044 mL 2.5221 mL 5.0443 mL
10 mM 0.2522 mL 1.2611 mL 2.5221 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 20% HP-β-CD in saline

    Solubility: 10 mg/mL (25.22 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.31 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.31 mM); Suspended solution

    此方案可获得 ≥ 2.5 mg/mL (6.31 mM,饱和度未知) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.31 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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