SY-5609 - CAS:2417302-07-7

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

目录号 : KM6715 CAS No. : 2417302-07-7 纯度 : 98%

Data Sheet 产品使用指南

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，K_D 为 0.065 nM。SY-5609 对 CDK2 (K_i=2600 nM)，CDK9 (K_i=960 nM)，CDK12 (K_i=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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

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

体外研究

SY-5609 (0.01-10000 nM; 72 hours) demonstrates strong antiproliferative effects in triple negative breast cancer (TNBC) and ovarian (OVA) cancer cells.
SY-5609 (100-500 nM; 48, 72 hours) induces apoptosis.
SY-5609 (100-500 nM; 48 hours) induces G2/M cell cycle arrest in HCC70 cells.
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.
SY-5609 (compound 101; 126.4 pM-4 µM; 72 hours) has an EC₅₀ of 5.6 nM in HCC70 cell line.

Cell Proliferation Assay

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

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

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

Western Blot Analysis

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

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

Animal Model:	Six-to-eight-week-old Balb/c nude female mice with HCC70 cell line
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.

分子式

C₂₃H₂₆F₃N₆OP

分子量

490.46

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。
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。