SY-5609 CDK7-IN-3|cas:2417302-07-7|西域试剂

SY-5609 CDK7-IN-3,99.66%

产品编号：Bellancom-138293| CAS NO：2417302-07-7| 分子式：C₂₃H₂₆F₃N₆OP| 分子量：490.46

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货号	价格	库存与货期
Bellancom-138293	￥5500.00	杭州北京（现货）
Bellancom-138293	￥9000.00	杭州北京（现货）
Bellancom-138293	￥18000.00	杭州北京（现货）

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SY-5609 CDK7-IN-3

产品介绍

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。

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.

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

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
(In Vivo)

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.

西域 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
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.

体内研究

西域 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
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.

体内研究

西域 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
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.

性状

Solid

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