2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. SNS-032

SNS-032  (Synonyms: BMS-387032)

目录号: HY-10008 纯度: 99.54%
COA 产品使用指南

摩尔计算器

SNS-032 (BMS-387032) 是一种有效的，选择性的 CDK2/7/9 抑制剂，IC50 值分别为 48 nM/62 nM/4 nM。SNS-032 具有抗肿瘤的功效。

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SNS-032 Chemical Structure

SNS-032 Chemical Structure

CAS No. : 345627-80-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550
In-stock
1 mg ￥250
In-stock
5 mg ￥500
In-stock
10 mg ￥700
In-stock
50 mg ￥1500
In-stock
100 mg ￥2500
In-stock
200 mg ￥4500
In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of SNS-032:

SNS-032 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

SNS-032 (BMS-387032) is a potent and selective inhibitor of CDK2, CDK7, and CDK9 with IC50s of 38 nM, 62 nM and 4 nM, respectively. SNS-032 has antitumor effect[1].

IC50 & Target[1]

CDK9

4 nM (IC50)

CDK2

38 nM (IC50)

CDK7

62 nM (IC50)

CDK1

480 nM (IC50)

CDK4

925 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CWR22R IC50
0.384 μM
Compound: 8; SNS032
Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay
Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay
[PMID: 35925880]
HCT-116 IC50
0.458 μM
Compound: 1, SNS-032
Inhibition of CDK9 in human HCT116 cells assessed as phosphor-ser2 level of RNA polymerase 2 after 16 hrs by high content cellular assay
Inhibition of CDK9 in human HCT116 cells assessed as phosphor-ser2 level of RNA polymerase 2 after 16 hrs by high content cellular assay
[PMID: 18842409]
HCT-116 IC50
0.55 μM
Compound: 1, SNS-032, BMS-387032
Inhibition of CDK9-mediated RNA pol 2 phosphorylation at ser2 in human HCT116 cells after 16 hrs by HCS assay
Inhibition of CDK9-mediated RNA pol 2 phosphorylation at ser2 in human HCT116 cells after 16 hrs by HCS assay
[PMID: 18926699]
HCT-116 IC50
0.7 μM
Compound: BMS-387032
Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay
[PMID: 30197029]
MCF7 IC50
1 μM
Compound: BMS-387032
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
[PMID: 30197029]
MOLT-4 IC50
173 nM
Compound: 13; SNS-032
Antiproliferative activity against human MOLT4 cells incubated for 72 hrs by cell titer glo assay
Antiproliferative activity against human MOLT4 cells incubated for 72 hrs by cell titer glo assay
[PMID: 32866383]
Sf9 IC50
21 nM
Compound: SNS032
Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA1 expressed in baculovirus infected Sf9 insect cells using FRET-labeled Ser/Thr 12 as substrate measured after 1 hr by Z'-lyte assay
Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA1 expressed in baculovirus infected Sf9 insect cells using FRET-labeled Ser/Thr 12 as substrate measured after 1 hr by Z'-lyte assay
[PMID: 32502343]
体外研究
(In Vitro)

SNS-032 has low sensitivity to CDK1 and CDK4 with IC50 of 480 nM and 925 nM, respectively. SNS-032 effectively kills chronic lymphocytic leukemia cells in vitro regardless of prognostic indicators and treatment history. Compared with flavopiridol and roscovitine, SNS-032 is more potent, both in inhibition of RNA synthesis and at induction of apoptosis. SNS-032 activity is readily reversible; removal of SNS-032 reactivates RNA polymerase II, which led to resynthesis of Mcl-1 and cell survival[1]. SNS-032 inhibits three dimensional capillary network formations of endothelial cells. SNS-032 completely prevents U87MG cell–mediated capillary formation of HUVECs. In addition, SNS-032 significantly prevents the production of VEGF in both cell lines, SNS-032 prevents in vitro angiogenesis, and this action is attributable to blocking of VEGF. Preclinical studies have shown that SNS-032 induces cell cycle arrest and apoptosis across multiple cell lines[2]. SNS-032 blocks the cell cycle via inhibition of CDKs 2 and 7, and transcription via inhibition of CDKs 7 and 9. SNS-032 activity is unaffected by human serum[3]. SNS-032 induces a dose-dependent increase in annexin V staining and caspase-3 activation. At the molecular level, SNS-032 induces a marked dephosphorylation of serine 2 and 5 of RNA polymerase (RNA Pol) II and inhibits the expression of CDK2 and CDK9 and dephosphorylated CDK7[5].

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

SNS-032 相关抗体:
体内研究
(In Vivo)

SNS-032 (15 mg/kg, i.p.) inhibits both xenografted BaF3-T674I cells and KBM5-T315I cells in vivo. SNS-032 abrogates the growth of tumors transplanted in nude mice with downregulation of T674I PDGFRα and T315I-Bcr-Abl[4].

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

380.53

Formula

C17H24N4O2S2
CAS 号
性状

固体

颜色

White to light yellow

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
细胞实验： 

DMSO 中的溶解度 : 62.5 mg/mL (164.24 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6279 mL 13.1396 mL 26.2791 mL
5 mM 0.5256 mL 2.6279 mL 5.2558 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

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

    Solubility: ≥ 2.08 mg/mL (5.47 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 2.08 mg/mL (5.47 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂： 50% PEG300    50% Saline

    Solubility: 10 mg/mL (26.28 mM); 悬浊液; 超声助溶

  • 方案 二

    请依序添加每种溶剂： 0.5% CMC-Na/saline water

    Solubility: 25 mg/mL (65.70 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.54%

COA (283 KB) RP-HPLC (261 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

Cell Titer-Glo (CTG) luminescent assay is performed to measure the growth curves of both HUVECs and U87MG cells. U87MG cells and HUVECs (2×103 cells/well) are seeded in a 96-well microplate in a final volume of 100 mL. After 24 hours, cells are treated with various doses of SNS-032 (0-0.5 mM) for 24, 48, or 72 hours. After completion of the treatment, 100 mL of CTG solution is added to each well and incubated for 20 minutes at room temperature in the dark. Lysate (50 mL) is transferred to a 96-well white plate, and luminescence is measured by POLARstar OPTIMA. Percent cell growth is calculated by considering 100% growth at the time of SNS-032 addition.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

Nude nu/nu BALB/c mice are housed in barrier facilities with a 12-hour light-dark cycle, with food and water available ad libitum. A mixture of 1×107 of BaF3-T674I cells with Matrigel or KBM5-T315I cells (3×107) are inoculated subcutaneously on the flanks of 4- to 6-week-old male nude mice. Tumors are measured every other day with use of calipers. Tumor volumes are calculated by the following formula: a2×b×0.4, where a is the smallest diameter and b is the diameter perpendicular to a. Four days after subcutaneous inoculation, when tumors are palpable (appr 100 mm3), mice are randomized to receive treatment with vehicle (tissue culture medium containing DMSO 0.1% v/v) or SNS-032 (15 mg/kg injected intraperitoneally every 2 days) for about 2 weeks. SNS-032 is dissolved in tissue culture grade DMSO before dilution. The body weight, feeding behavior, and motor activity of each animal are monitored as indicators of general health. The animals are then euthanized, and tumor xenografts are immediately removed, weighed, stored, and fixed.

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

SNS-032 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6279 mL 13.1396 mL 26.2791 mL 65.6978 mL
5 mM 0.5256 mL 2.6279 mL 5.2558 mL 13.1396 mL
10 mM 0.2628 mL 1.3140 mL 2.6279 mL 6.5698 mL
15 mM 0.1752 mL 0.8760 mL 1.7519 mL 4.3799 mL
20 mM 0.1314 mL 0.6570 mL 1.3140 mL 3.2849 mL
25 mM 0.1051 mL 0.5256 mL 1.0512 mL 2.6279 mL
30 mM 0.0876 mL 0.4380 mL 0.8760 mL 2.1899 mL
40 mM 0.0657 mL 0.3285 mL 0.6570 mL 1.6424 mL
50 mM 0.0526 mL 0.2628 mL 0.5256 mL 1.3140 mL
60 mM 0.0438 mL 0.2190 mL 0.4380 mL 1.0950 mL
80 mM 0.0328 mL 0.1642 mL 0.3285 mL 0.8212 mL
100 mM 0.0263 mL 0.1314 mL 0.2628 mL 0.6570 mL
Help & FAQs
  • 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:

SNS-032345627-80-7BMS-387032SNS032SNS 032BMS387032BMS 387032CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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