| 规格 | 价格 | |
|---|---|---|
| 50mg | ||
| 100mg | ||
| Other Sizes |
| 参考文献 | |
|---|---|
| 其他信息 |
LSM-1131 属于吲哚类化合物。
替万替尼已在实体瘤中进行过研究。 替万替尼是一种口服生物利用度高的小分子 c-Met 抑制剂,具有潜在的抗肿瘤活性。c-Met 抑制剂 ARQ 197 与 c-Met 蛋白结合,破坏 c-Met 信号转导通路,这可能诱导过表达 c-Met 蛋白或组成型激活 c-Met 蛋白的肿瘤细胞死亡。c-Met 蛋白是原癌基因 c-Met 的产物,是一种受体酪氨酸激酶,也称为肝细胞生长因子受体 (HGFR)。这种蛋白质在多种肿瘤细胞类型中过度表达或发生突变,并在肿瘤细胞增殖、存活、侵袭、转移和肿瘤血管生成中发挥关键作用。 药物适应症 治疗肝母细胞瘤 作用机制 替万替尼通过抑制c-Met的活性发挥作用。c-Met是一种受体酪氨酸激酶,在人类癌症中发挥多种关键作用,包括癌细胞生长、存活、血管生成、侵袭和转移。c-Met在大多数癌症中异常激活,被认为控制着参与肿瘤生长和转移的多种信号转导通路。 |
| 分子式 |
C23H19N3O2
|
|---|---|
| 分子量 |
369.415865182877
|
| 精确质量 |
369.147
|
| CAS号 |
905853-99-8
|
| 相关CAS号 |
Tivantinib;905854-02-6;(3S,4S)-Tivantinib;905854-03-7;(Rac)-Tivantinib;1239986-50-5
|
| PubChem CID |
11494412
|
| 外观&性状 |
Off-white to pink solid powder
|
| 密度 |
1.49±0.1 g/cm3(Predicted)
|
| 沸点 |
715.9±60.0 °C(Predicted)
|
| 闪点 |
386.8±32.9 °C
|
| 蒸汽压 |
0.0±2.3 mmHg at 25°C
|
| 折射率 |
1.797
|
| LogP |
3.26
|
| tPSA |
66.9
|
| 氢键供体(HBD)数目 |
2
|
| 氢键受体(HBA)数目 |
2
|
| 可旋转键数目(RBC) |
2
|
| 重原子数目 |
28
|
| 分子复杂度/Complexity |
666
|
| 定义原子立体中心数目 |
2
|
| SMILES |
O=C1NC(=O)[C@@H](C2=CNC3C=CC=CC2=3)[C@@H]1C1=CN2CCCC3C2=C1C=CC=3
|
| InChi Key |
UCEQXRCJXIVODC-PMACEKPBSA-N
|
| InChi Code |
InChI=1S/C23H19N3O2/c27-22-19(16-11-24-18-9-2-1-7-14(16)18)20(23(28)25-22)17-12-26-10-4-6-13-5-3-8-15(17)21(13)26/h1-3,5,7-9,11-12,19-20,24H,4,6,10H2,(H,25,27,28)/t19-,20-/m0/s1
|
| 化学名 |
(3R,4R)-3-(1-azatricyclo[6.3.1.04,12]dodeca-2,4,6,8(12)-tetraen-3-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 溶解度 (体外实验) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 溶解度 (体内实验) |
注意: 如下所列的是一些常用的体内动物实验溶解配方,主要用于溶解难溶或不溶于水的产品(水溶度<1 mg/mL)。 建议您先取少量样品进行尝试,如该配方可行,再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80: Saline = 10 : 5 : 85 (如: 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备:将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中,得到澄清溶液。 注射用配方 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (如: 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如: 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液,加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如:100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中,得到0.5%CMC-Na澄清溶液;然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中,得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 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 | 2.7069 mL | 13.5347 mL | 27.0695 mL | |
| 5 mM | 0.5414 mL | 2.7069 mL | 5.4139 mL | |
| 10 mM | 0.2707 mL | 1.3535 mL | 2.7069 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) 。
Link: https://clinicaltrials.gov/ct2/show/NCT06987942
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Conditions:Carcinoma, Small Cell
Title:Study of Tivantinib (ARQ 197) Plus Cetuximab in EGFR Inhibitor-Resistant MET High Subjects
Status:Completed
updateDate:2022-09-09
Ctid:NCT01892527
Link: https://clinicaltrials.gov/ct2/show/NCT01892527
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Conditions:Solid TumorLink: https://clinicaltrials.gov/ct2/show/NCT01075048
Conditions:Metastatic Colorectal CancerLink: https://clinicaltrials.gov/ct2/show/NCT01244191
Conditions:Non Squamous, Non-small-cell Lung CancerLink: https://clinicaltrials.gov/ct2/show/NCT01055067
Conditions:Non-CNS Germ Cell Tumors (Seminomas and Nonseminomas)Link: https://clinicaltrials.gov/ct2/show/NCT01755767
Conditions:Hepatocellular CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT01178411
Conditions:Advanced Solid TumorsLink: https://clinicaltrials.gov/ct2/show/NCT02049060
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Conditions:Refractory Multiple MyelomaLink: https://clinicaltrials.gov/ct2/show/NCT02150733
Conditions:Hepatic Impairment|Solid Tumor|CancerLink: https://clinicaltrials.gov/ct2/show/NCT01699061
Conditions:Solid TumorsLink: https://clinicaltrials.gov/ct2/show/NCT01517399
Conditions:Solid TumorsLink: https://clinicaltrials.gov/ct2/show/NCT01149720
Conditions:Solid TumorsLink: https://clinicaltrials.gov/ct2/show/NCT01688973
Conditions:Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT01696955
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Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT01519414
Conditions:Hormone-Resistant Prostate Cancer|Prostate Adenocarcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate CancerLink: https://clinicaltrials.gov/ct2/show/NCT01654965
Conditions:Adult Solid NeoplasmLink: https://clinicaltrials.gov/ct2/show/NCT01749384
Conditions:Solid NeoplasmLink: https://clinicaltrials.gov/ct2/show/NCT02029157
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Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT03022422
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Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT02188810
Conditions:FluLink: https://clinicaltrials.gov/ct2/show/NCT01625156
Conditions:Adult Solid NeoplasmLink: https://clinicaltrials.gov/ct2/show/NCT01580735
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Conditions:Influenza ALink: https://clinicaltrials.gov/ct2/show/NCT01014806
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Conditions:Cancer, Advanced Solid TumorsLink: https://clinicaltrials.gov/ct2/show/NCT00612703
Conditions:CancerLink: https://clinicaltrials.gov/ct2/show/NCT00802555
Conditions:Cirrhosis|Hepatocellular CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT00569894
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT00192322
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT00492557
Conditions:Pneumococcal InfectionsLink: https://clinicaltrials.gov/ct2/show/NCT00192309
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Conditions:HealthyLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2009-016025-34
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