规格 | 价格 | 库存 | 数量 |
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2mg |
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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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靶点 |
Smoothened
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体外研究 (In Vitro) |
体外活性:LY2940680 抑制含有编码 Smoothened 基因突变的细胞系中的癌症生长,研究人员之前在对 vismodegib 产生耐药性的癌症患者中观察到这一点。激酶测定:Taladegib 是一种平滑受体的小分子拮抗剂,对细胞增殖显示出轻微的抑制作用,在粘蛋白(IC50:Taladegib=49.8±4.5 μM)和混合胆管癌(CCA)(IC50:Taladegib= 61.2±21.1μM)。细胞测定:当使用含有编码 Smoothened 的基因突变的细胞系进行测试时,研究人员之前在对 vismodegib 产生耐药性的癌症患者中观察到,LY2940680 抑制了细胞增殖。
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体内研究 (In Vivo) |
LY2940680 在啮齿类和非啮齿类动物中具有优异的药代动力学特性。 LY2940680口服治疗Ptch+/-p53-/-转基因小鼠自发发生髓母细胞瘤,疗效显着,并显着提高其生存率。通过这些小鼠的磁共振成像,LY2940680 揭示了抗肿瘤活性的快速动力学,并且通过髓母细胞瘤的免疫组织化学分析,LY2940680 诱导 Caspase-3 活性并减少增殖。 LY2940680 抑制皮下异种移植肿瘤基质中 Hh 调节的基因表达,并产生显着的抗肿瘤活性。
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动物实验 |
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参考文献 |
分子式 |
C26H24F4N6O
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分子量 |
512.5
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精确质量 |
512.19
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元素分析 |
C, 60.93; H, 4.72; F, 14.83; N, 16.40; O, 3.12
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CAS号 |
1258861-20-9
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相关CAS号 |
1258861-20-9; 1258861-21-0 (HCl)
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外观&性状 |
White solid powder
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SMILES |
CN1C(=CC=N1)C2=NN=C(C3=CC=CC=C32)N4CCC(CC4)N(C)C(=O)C5=C(C=C(C=C5)F)C(F)(F)F
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InChi Key |
SZBGQDXLNMELTB-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C26H24F4N6O/c1-34(25(37)20-8-7-16(27)15-21(20)26(28,29)30)17-10-13-36(14-11-17)24-19-6-4-3-5-18(19)23(32-33-24)22-9-12-31-35(22)2/h3-9,12,15,17H,10-11,13-14H2,1-2H3
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化学名 |
4-fluoro-N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoromethyl)benzamide
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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 (4.88 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 (4.88 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 (4.88 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 | 1.9512 mL | 9.7561 mL | 19.5122 mL | |
5 mM | 0.3902 mL | 1.9512 mL | 3.9024 mL | |
10 mM | 0.1951 mL | 0.9756 mL | 1.9512 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 |
NCT05199584 | Active Recruiting |
Drug: ENV-101 (taladegib) |
Solid Tumors With PTCH1 Loss-of-function Mutations |
Endeavor Biomedicines, Inc. | May 24, 2022 | Phase 2 |
NCT04968574 | Active Recruiting |
Drug: taladegib Drug: placebo |
Idiopathic Pulmonary Fibrosis | Endeavor Biomedicines, Inc. | August 26, 2021 | Phase 2 |
NCT05817240 | Completed | Drug: taladegib Drug: nintedanib |
Idiopathic Pulmonary Fibrosis | Endeavor Biomedicines, Inc. | May 3, 2023 | Phase 1 |
NCT01226485 | Completed | Drug: Taladegib | Advanced Cancer | Eli Lilly and Company | September 2010 | Phase 1 |
NCT02784795 | Completed | Drug: Taladegib Drug: Abemaciclib |
Solid Tumor Breast Cancer |
Eli Lilly and Company | November 4, 2016 | Phase 1 |
Effect of Sonic Hedgehog (Hg) pathway inhibitors on proliferation and apoptosis of mucin and mixed CCA primary cultures.PLoS One.2015 Nov 16;10(11):e0142124. th> |
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