SY-5609(Synonyms: CDK7-IN-3)

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SY-5609 (Synonyms: CDK7-IN-3) 纯度: 99.66%

SY-5609 (CDK7-IN-3) 是一种口服有效的，高选择性，非共价的 CDK7 抑制剂，KD 为 0.065 nM。SY-5609 对 CDK2 (Ki=2600 nM)，CDK9 (Ki=960 nM)，CDK12 (Ki=870 nM) 具有较弱的抑制作用。SY-5609 诱导肿瘤细胞凋亡并具有抗肿瘤活性。

SY-5609(Synonyms: CDK7-IN-3)

SY-5609 Chemical Structure

CAS No. : 2417302-07-7

规格 价格 是否有货 数量
5 mg ￥5500 In-stock
10 mg ￥9000 In-stock
25 mg ￥18000 In-stock
50 mg   询价  
100 mg   询价  

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SY-5609 相关产品

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生物活性

SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (Ki=2600 nM), CDK9 (Ki=960 nM), CDK12 (Ki=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity[1][2].

IC50 & Target[1]

CDK7

0.065 nM (Kd)

CDK2

2600 nM (Ki)

CDK9

960 nM (Ki)

CDK12

870 nM (Ki)

体外研究
(In Vitro)

SY-5609 (0.01-10000 nM; 72 hours) demonstrates strong antiproliferative effects in triple negative breast cancer (TNBC) and ovarian (OVA) cancer cells[1].
SY-5609 (100-500 nM; 48, 72 hours) induces apoptosis[1].
SY-5609 (100-500 nM; 48 hours) induces G2/M cell cycle arrest in HCC70 cells[1].
SY-5609 (25-500 nM; 6-48 hours) results in inhibition of the phosphorylation of CDK2 at Thr160 via loss of CAK function for 24 and 48 h[1].
SY-5609 (compound 101; 126.4 pM-4 µM; 72 hours) has an EC50 of 5.6 nM in HCC70 cell line[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HCC70, MDA-MB453, COV504, A2780, OVCAR3, CAOV3 cells
Concentration: 0.01-10000 nM
Incubation Time: 72 hours
Result: Demonstrated strong antiproliferative effects with IC50 of 1-6 nM.

Apoptosis Analysis[1]

Cell Line: HCC70, MDA-MB-468, CAOV3 and OVCAR3 cells
Concentration: 100, 250, 500 nM
Incubation Time: 48 and 72 hours
Result: Induced apoptosis.

Cell Cycle Analysis[1]

Cell Line: HCC70 cells
Concentration: 100, 250, 500 nM
Incubation Time: 48 hours
Result: Induced G2/M cell cycle arrest.

Western Blot Analysis[1]

Cell Line: HCC70 cells
Concentration: 25, 50, 100, 250, 500 nM
Incubation Time: 6, 24, 48 hours
Result: Resulted in inhibition of the phosphorylation of CDK2 at Thr160 via loss of CAK function for 24 and 48 h.

体内研究
(In Vivo)

SY-5609 (2 mg/kg/day; orally; for 21 days) induces tumor regression over the 21-day dosing period[1].
Daily oral dosing of 2 mg/kg SY-5609 in mice provided a plasma exposure of 261.28 ng h/mL with a Cmax of 50.67 ng/mL (103 nM) and an elimination half-life of 3.33 h[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-to-eight-week-old Balb/c nude female mice with HCC70 cell line[1]
Dosage: 2 mg/kg
Administration: Orally; daily; for 21 days
Result: Induced tumor regression over the 21-day dosing period and was well tolerated. No regrowth of tumor was observed out to day 28.

分子量

490.46

Formula

C23H26F3N6OP
CAS 号

2417302-07-7
运输条件

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

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 40 mg/mL (81.56 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0389 mL 10.1945 mL 20.3890 mL
5 mM 0.4078 mL 2.0389 mL 4.0778 mL
10 mM 0.2039 mL 1.0195 mL 2.0389 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 (stored under nitrogen)。-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： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 4 mg/mL (8.16 mM); Suspended solution; Need ultrasonic

    此方案可获得 4 mg/mL (8.16 mM) 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 40.0 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

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

    Solubility: ≥ 4 mg/mL (8.16 mM); Clear solution

    此方案可获得 ≥ 4 mg/mL (8.16 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 40.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.10 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Jason J Marineau, et al. Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7. J Med Chem. 2021 Nov 2.

    [2]. Michael Bradley, et al. Inhibitors of cyclin-dependent kinase 7 (cdk7). WO2020093011A1.

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