NU 6102是一种强效的CDK1和CDK2抑制剂，对CDK1/cyclin B和CDK2/cyclin A3的IC50值分别为9.5nM和5.4nM。
Cas No.:444722-95-6
Sample solution is provided at 25 µL, 10mM.
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NU 6102 is a potent CDK1 and CDK2 inhibitor with IC50 values of 9.5nM and 5.4nM for CDK1/cyclin B and CDK2/cyclin A3, respectively [1]. NU 6102 can induce the G2 arrest, inhibition of Rb phosphorylation, and cytotoxicity [2]. NU 6102 has been widely used to delay the growth of tumors in mice and inhibit the progression of xenograft tumors[3].
In vitro, NU 6102 treatment (10µM) for 72 hours significantly inhibited the proliferation of HCT116 cells[4]. Treatment with 25µM NU 6102 for 48 hours significantly increased the expression of p21 protein in BT483 cells and decreased the expression of Erb2 protein, and led to a significant decrease in cell viability[5]. Treatment with 25µM NU 6102 for 24 hours reduced the level of Mcl-1 and enhanced the apoptosis of chronic lymphocytic leukemia (CLL) cells mediated by LBH589[6].
In vivo, NU 6102 treatment via intraperitoneal injection at a dose of 100mg/kg twice daily for 10 days reduced the tumor volume in mice with HT29 xenografts[4].
References:
[1] Hardcastle I R, Arris C E, Bentley J, et al. N2-substituted O 6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2[J]. Journal of medicinal chemistry, 2004, 47(15): 3710-3722.
[2] Anscombe E, Meschini E, Mora-Vidal R, et al. Identification and characterization of an irreversible inhibitor of CDK2[J]. Chemistry & biology, 2015, 22(9): 1159-1164.
[3] Newell D, Thomas H, Wang L, et al. Preclinical in vitro and in vivo evaluation of the cyclin dependent kinase 2 inhibitor NU6102 and a water pro-drug NU6301[J]. Cancer Research, 2008, 68(9_Supplement): 2413-2413.
[4] Beale G, Haagensen E J, Thomas H D, et al. Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo antitumour activity in colorectal cancer[J]. British journal of cancer, 2016, 115(6): 682-690.
[5] Chuang P Y, Huang C, Huang H C. The use of a combination of tamoxifen and doxorubicin synergistically to induce cell cycle arrest in BT483 cells by down-regulating CDK1, CDK2 and cyclin D expression[J]. Journal of Pharmaceutical Technology and Drug Research, 2013, 2(1): 12.
[6] Inoue S, Walewska R, Dyer M J S, et al. Downregulation of Mcl-1 potentiates HDACi-mediated apoptosis in leukemic cells[J]. Leukemia, 2008, 22(4): 819-825.
NU 6102是一种强效的CDK1和CDK2抑制剂，对CDK1/cyclin B和CDK2/cyclin A3的IC50值分别为9.5nM和5.4nM[1]。NU 6102可诱导G2期阻滞、抑制Rb磷酸化并产生细胞毒性[2]。NU 6102已被广泛用于延缓小鼠肿瘤生长并抑制异种移植肿瘤的进展[3]。
在体外，使用10μM的NU 6102处理HCT116细胞72小时，显著抑制了细胞增殖[4]。使用25μM的NU 6102处理BT483细胞48小时，显著增加了p21蛋白的表达，降低了Erb2蛋白的表达，并导致细胞活力显著下降[5]。使用25μM的NU 6102处理24小时，可降低慢性淋巴细胞白血病(CLL)细胞中Mcl-1的水平，并增强LBH589介导的细胞凋亡[6]。
在体内，每日两次腹腔注射100mg/kg剂量的NU 6102，连续10天，减少了携带HT29异种移植瘤小鼠的肿瘤体积[4]。
| Cell experiment [1]: | |
Cell lines | BT483 cells |
Preparation Method | BT483 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum (FBS), 1% penicillin-streptomycin at 37℃ in the presence of 5% CO2. Cells were seeded at 2×104 cells/well in a 24-well flat-bottomed plate for 24h, treated with varying concentrations of NU 6102 (0, 1, 2, 5, 10, 15, and 20µM) and incubated for an additional 48h, then analyzed the cell viability. |
Reaction Conditions | 0, 1, 2, 5, 10, 15, and 20µM; 48h |
Applications | NU 6102 treatment significantly reduced the cell viability of BT483 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | CD-1 nude mice |
Preparation Method | CD-1 nude mice (6-week-old) were housed in temperature (23±2°C) and light-controlled (12:12-hour light-dark cycle) animal care facility. D-1 nude mice were implanted with 1×107 HT29 cells, in a mixture of Matrigel/RPMI cell culture media (1:1 v/v), subcutaneously on the right flank. Mice were treated with vehicle (control), NU 6102 100mg/kg i.p., twice daily for 10 days. Tumor volume was calculated from two-dimensional calliper measurements using the equation a2×b/2, where a is the smallest measurement and b the largest. |
Dosage form | 100mg/kg; twice daily for 10 days; i.p. |
Applications | NU 6102 treatment reduced tumor volume in mice with HT29 xenografts. |
References: | |
| Cas No. | 444722-95-6 | SDF | |
| 别名 | 4-[[6-(环己基甲氧基)-1H-嘌呤-2-基]氨基]苯磺酰胺 | ||
| 化学名 | 4-[[6-(cyclohexylmethoxy)-9H-purin-2-yl]amino]-benzenesulfonamide | ||
| Canonical SMILES | NS(C(C=C1)=CC=C1NC2=NC(NC=N3)=C3C(OCC4CCCCC4)=N2)(=O)=O | ||
| 分子式 | C18H22N6O3S | 分子量 | 402.5 |
| 溶解度 | DMSO: >1 mg/ml,Ethanol: >1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4845 mL | 12.4224 mL | 24.8447 mL |
| 5 mM | 496.9 μL | 2.4845 mL | 4.9689 mL |
| 10 mM | 248.4 μL | 1.2422 mL | 2.4845 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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