规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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1mg |
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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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体外研究 (In Vitro) |
ENMD-2076 针对 Aurora A 而非 Aurora B (IC50=350 nM)。 ENMD-2076 抑制 HUVEC 增殖,IC50 为 0.15 mM。 10 种人类白血病细胞系的 IC50 值范围为 0.025 至 0.53 mM。在该图中,MV4:11 细胞的反应性最强,其反应系数超过 4 倍。用 ENMD-2076 处理的淋巴瘤来源的 U937 细胞系显示 G2-M 期停滞和细胞凋亡呈剂量依赖性增加。 ENMD-2076 抑制 THP-1 细胞中细胞 Flt3 配体 (FL) 诱导的 Flt3 自磷酸化,该细胞已被证明表达 FL 响应性野生型 Flt-3 (18),IC50 为 28 nM。 ENMD-2076 抑制 MO7e 细胞中干细胞因子 (SCF) 诱导的 Kit 自磷酸化,IC50 为 40 nM。 ENMD-2076 抑制 VEGFR2/KDR 自磷酸化,IC50 为 7 nM [1]。
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体内研究 (In Vivo) |
ENMD-2076 治疗可导致统计学上显着的肿瘤生长或消退抑制,且呈剂量依赖性。此外,由于ENMD-2076对快速生长的肿瘤(如A375黑色素瘤)和缓慢生长的肿瘤(如HT29结肠癌)的抑制作用类似,因此肿瘤生长速率和抗肿瘤功效之间不存在相关性,而这在理论上是有丝分裂激酶抑制剂所预期的。除 A375 模型外,研究尚未发现 ENMD-2076 每日剂量高达 302 mg/kg(相当于 200 mg/kg 游离碱)有任何体重减轻或发病迹象。
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动物实验 |
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参考文献 |
[1]. Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37.
[2]. Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25 |
分子式 |
C21H25N7
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分子量 |
375.470103025436
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CAS号 |
934353-76-1
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相关CAS号 |
ENMD-2076 Tartrate;1453868-32-0
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SMILES |
CN1CCN(C2=CC(NC3=NNC(C)=C3)=NC(/C=C/C4=CC=CC=C4)=N2)CC1
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InChi Key |
BLQYVHBZHAISJM-CMDGGOBGSA-N
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InChi Code |
InChI=1S/C21H25N7/c1-16-14-20(26-25-16)23-19-15-21(28-12-10-27(2)11-13-28)24-18(22-19)9-8-17-6-4-3-5-7-17/h3-9,14-15H,10-13H2,1-2H3,(H2,22,23,24,25,26)/b9-8+
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化学名 |
(E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine.
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别名 |
ENMD 2076; ENMD-2076; ENMD2076.
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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 |
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 (6.66 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 (6.66 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (6.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% CMC+0.25% Tween 80:30mg/mL 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 | 2.6633 mL | 13.3166 mL | 26.6333 mL | |
5 mM | 0.5327 mL | 2.6633 mL | 5.3267 mL | |
10 mM | 0.2663 mL | 1.3317 mL | 2.6633 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) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00806065 | Completed | Drug: ENMD-2076 | Multiple Myeloma | CASI Pharmaceuticals, Inc. | December 2008 | Phase 1 |
NCT00904787 | Completed | Drug: ENMD-2076 | Relapsed or Refractory Hematological Malignancies |
CASI Pharmaceuticals, Inc. | April 2009 | Phase 1 |
NCT01104675 | Completed | Drug: ENMD-2076 | Ovarian Cancer Fallopian Cancer |
CASI Pharmaceuticals, Inc. | April 2010 | Phase 2 |
NCT00658671 | Completed | Drug: ENMD-2076 | Advanced Cancer | CASI Pharmaceuticals, Inc. | April 2008 | Phase 1 |
Antiangiogenic action of ENMD-2076. Mol Cancer Ther. 2011 Jan;10(1):126-37. td> |
ENMD-2076 inhibits Flt3, VEGFR2/KDR, FGFR-1/2, and Aurora A in vivo. Mol Cancer Ther. 2011 Jan;10(1):126-37. td> |
ENMD-2076 inhibits blood vessel formation and impacts the growth of established MDA-MB-231 tumors. Mol Cancer Ther. 2011 Jan;10(1):126-37. td> |