| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| 靶点 |
JNK3 (IC50 = 6 nM); JNK2 (IC50 = 7 nM); JNK1 (IC50 = 61 nM)
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|---|---|
| 体外研究 (In Vitro) |
Tanzisertib (CC-930) 抑制 phorbol-12-myristate-13-acetate 和植物血凝素刺激的人 PBMC 中磷酸-cJun 的合成 (IC50=1 μM)[1]。在 FC 负载的 WT 肝细胞中，tanzisertib (CC-930) (1-2 μM) 完全消除细胞凋亡和坏死[2]。在系统性硬化症中，tanzisertib (CC-930) 抑制由促纤维化细胞因子触发的 JNK 通路[3]。
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| 体内研究 (In Vivo) |
在急性大鼠 LPS 诱导的 TNFa 产生 PK-PD 模型中，Tanzisertib (CC-930)（10 和 30 mg/kg，口服）可抑制 TNFa 的产生 23% 和 77%[1]。 Tanzisertib (CC-930) (150 mg/kg) 可以使先前存在的纤维化消退，同时还可以防止各种模型中纤维化的发展[3]。
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| 酶活实验 |
CC-930 在蛋白质底物 c-Jun 的 JNK 依赖性磷酸化中与 ATP 具有动力学竞争性，并且对所有 JNK 亚型有效 [Ki(JNK1) = 44 ± 3 nM，IC50(JNK1) = 61 nM，Ki(JNK2) ) = 6.2 ± 0.6 nM，IC50(JNK2) = 5 nM，IC50(JNK3) = 5 nM]，对 MAP 激酶 ERK1 和 p38a 具有选择性，IC50 分别为 0.48 和 3.4 μM。
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| 细胞实验 |
在含有 1 µM Tanzisertib (CC-930) 的 96 孔板中，将来自系统性硬化症 (SSc) 患者的成纤维细胞孵育 20 小时。然后将细胞在 37°C 下再孵育 4 小时，然后接受终浓度为 1 mg/mL 的 MTT。所有其他结果均针对未处理的细胞进行标准化，而模拟处理的成纤维细胞作为标准。
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| 动物实验 |
A modified version of the bleomycin-induced dermal fibrosis model is used to assess the regression of fibrosis on inhibition of JNK. In this model, significant dermal fibrosis is already present three weeks after the start of the challenge and is treated with bleomycin. The results of six different groups, comprising a total of 40 mice, are analyzed. NaCl is subcutaneously injected into the first group of mice for a total of six weeks. In order to assess the level of fibrosis prior to treatment and to prevent spontaneous fibrosis regression, the second group receives injections of bleomycin for 3 weeks, followed by injections of NaCl for an additional 3 weeks. After six weeks of bleomycin injections, the third group of mice is euthanized. The final three weeks of a continuous six-week challenge with bleomycin are spent administering Tanzisertib (CC-930) to the fourth and fifth groups at doses of 50 mg/kg and 150 mg/kg, respectively. The sixth group is a positive control group made up of mice that were given bleomycin for six weeks before being given imatinib at a dose of 50 mg/kg for the final three weeks.
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| 参考文献 |
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| 分子式 |
C21H23F3N6O2
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|---|---|---|
| 分子量 |
448.44
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| 精确质量 |
448.18
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| 元素分析 |
C, 56.24; H, 5.17; F, 12.71; N, 18.74; O, 7.14
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| CAS号 |
899805-25-5
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| 相关CAS号 |
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| 外观&性状 |
White to off-white solid powder
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| SMILES |
C1COC[C@H]1N2C3=NC(=NC=C3N=C2NC4=C(C=C(C=C4F)F)F)NC5CCC(CC5)O
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| InChi Key |
IBGLGMOPHJQDJB-MOKVOYLWSA-N
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| InChi Code |
InChI=1S/C21H23F3N6O2/c22-11-7-15(23)18(16(24)8-11)28-21-27-17-9-25-20(26-12-1-3-14(31)4-2-12)29-19(17)30(21)13-5-6-32-10-13/h7-9,12-14,31H,1-6,10H2,(H,27,28)(H,25,26,29)/t12?,13-,14?/m0/s1
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| 化学名 |
4-[[9-[(3S)-oxolan-3-yl]-8-(2,4,6-trifluoroanilino)purin-2-yl]amino]cyclohexan-1-ol
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| 别名 |
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
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| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2300 mL | 11.1498 mL | 22.2995 mL | |
| 5 mM | 0.4460 mL | 2.2300 mL | 4.4599 mL | |
| 10 mM | 0.2230 mL | 1.1150 mL | 2.2300 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
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 ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
JNK3 inhibitor-6
JNK-1-IN-2
JNK-IN-12
JIP-1(153-163) TFA (T1-JIP TFA)
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