NVP-TNKS656
(Synonyms: TNKS656) 目录号 : GC17555
A TNKS2 inhibitor
Cas No.:1419949-20-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Athymic female nude mice weighing 19-22 g are implanted subcutaneously with a 3×3×3 mm3 tumor fragment from an MMTV-Wnt1 tumor-bearing mouse. Tumors are grown to approximately 250-300 mm3. Individual mice are given a single oral dose of vehicle (n=3) (4% HCl:10% propylene glycol:20% Solutol HS15:60.5% D5W:0.5% NaOH) or TNKS656 at 350 mg/kg (n=18). At 0.5, 1, 2, 4, 8, 16, or 24 h following dosing (n=3/time point), mice are euthanized, and blood is collected via cardiac puncture and processed for plasma. Tumors are excised from mice and frozen at −80°C for PD analysis. |
References: [1]. Shultz MD, et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor. J Med Chem. 2013 Aug 22;56(16):6495-511. | |
NVP-TNKS656 is an orally active antagonist of Wnt pathway activity. The Wnt pathway has been involved in controlling numerous developmental processes. Dysfunction of this pathway may result in carcinogenesis [1].
In vitro: The IC50 value of NVP-TNKS656 against PARP1, TNKS2, PARP2, and STF was > 19, 0.006, 32, and 0.0035 µM, respectively [1].
In vivo: The clearance and volume of distribution of NVP-TNKS656 were 10 mL/min/kg and 0.6 L/kg after intravenous administration in mice. The exposure and oral bioavailability was 32% and 53%, respectively. In the mouse mammary tumor virus (MMTV)-Wnt1 transgenic model, oral administration of NVP-TNKS656 (350 mg/kg) activated the Wnt signaling over a 24-h time course. NVP-TNKS656 treatment reduced the Wnt/beta-catenintarget gene Axin2 mRNA level by 70-80% [1].
Reference:
Shultz M D, Cheung A K, Kirby C A, et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor[J]. Journal of medicinal chemistry, 2013, 56(16): 6495-6511.
| Cas No. | 1419949-20-4 | SDF | |
| 别名 | TNKS656 | ||
| 化学名 | N-(cyclopropylmethyl)-N-((4-hydroxy-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)methyl)-2-(4-(4-methoxybenzoyl)piperidin-1-yl)acetamide | ||
| Canonical SMILES | COC1=CC=C(C(C2CCN(CC(N(CC3=NC4=C(C(O)=N3)COCC4)CC5CC5)=O)CC2)=O)C=C1 | ||
| 分子式 | C27H34N4O5 | 分子量 | 494.58 |
| 溶解度 | DMF: 33 mg/ml,DMSO: 33 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.20 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0219 mL | 10.1096 mL | 20.2192 mL |
| 5 mM | 0.4044 mL | 2.0219 mL | 4.0438 mL |
| 10 mM | 0.2022 mL | 1.011 mL | 2.0219 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。