| Size | Price | |
|---|---|---|
| 50mg | ||
| 100mg | ||
| Other Sizes |
| References | |
|---|---|
| Additional Infomation |
LSM-1131 belongs to the indole class of compounds. Tevlantinib has been studied in solid tumors. Tevlantinib is a small-molecule c-Met inhibitor with high oral bioavailability and potential anti-tumor activity. The c-Met inhibitor ARQ 197 binds to the c-Met protein, disrupting the c-Met signaling pathway, which may induce death in tumor cells overexpressing or constitutively activating c-Met protein. c-Met protein is a product of the proto-oncogene c-Met, a receptor tyrosine kinase also known as the hepatocyte growth factor receptor (HGFR). This protein is overexpressed or mutated in various tumor cell types and plays a crucial role in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis. Drug Indications: Treatment of hepatoblastoma. Mechanism of Action: Tevlantinib exerts its effect by inhibiting c-Met activity. c-Met is a receptor tyrosine kinase that plays multiple key roles in human cancers, including cancer cell growth, survival, angiogenesis, invasion, and metastasis. c-Met is aberrantly activated in most cancers and is believed to control multiple signal transduction pathways involved in tumor growth and metastasis.
|
| Molecular Formula |
C23H19N3O2
|
|---|---|
| Molecular Weight |
369.415865182877
|
| Exact Mass |
369.147
|
| CAS # |
905853-99-8
|
| Related CAS # |
Tivantinib;905854-02-6;(3S,4S)-Tivantinib;905854-03-7;(Rac)-Tivantinib;1239986-50-5
|
| PubChem CID |
11494412
|
| Appearance |
Off-white to pink solid powder
|
| Density |
1.49±0.1 g/cm3(Predicted)
|
| Boiling Point |
715.9±60.0 °C(Predicted)
|
| Flash Point |
386.8±32.9 °C
|
| Vapour Pressure |
0.0±2.3 mmHg at 25°C
|
| Index of Refraction |
1.797
|
| LogP |
3.26
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
28
|
| Complexity |
666
|
| Defined Atom Stereocenter Count |
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
|
| Chemical Name |
(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
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
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
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT06987942
Conditions:Varicella|Influenza VaccineLink: https://clinicaltrials.gov/ct2/show/NCT02868970
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT02608411
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
Conditions:Colorectal Cancer Metastatic|C-met OverexpressionLink: https://clinicaltrials.gov/ct2/show/NCT01676402
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT01468922
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
Conditions:Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of LungLink: https://clinicaltrials.gov/ct2/show/NCT01447914
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
Conditions:Head and Neck Squamous Cell Carcinoma|Recurrent Head and Neck CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT01609998
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
Conditions:Liver CancerLink: https://clinicaltrials.gov/ct2/show/NCT01682369
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT03022422
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT03022435
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT01998477
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT01152645
Conditions:Gastric CancerLink: https://clinicaltrials.gov/ct2/show/NCT01656265
Conditions:Advanced Hepatocellular CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT01611857
Conditions:Malignant Solid Tumour|Gastroesophageal CancerLink: https://clinicaltrials.gov/ct2/show/NCT01861301
Conditions:Epithelioid Mesothelioma|Recurrent Malignant Mesothelioma|Sarcomatoid Mesothelioma|Stage II Pleural Mesothelioma|Stage III Pleural Mesothelioma|Stage IV Pleural MesotheliomaLink: https://clinicaltrials.gov/ct2/show/NCT02307851
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT01498718
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT01575522
Conditions:Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer|Triple-Negative Breast CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT02293317
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
Conditions:Non-small-cell Lung CancerLink: https://clinicaltrials.gov/ct2/show/NCT01725191
Conditions:Childhood Solid NeoplasmLink: https://clinicaltrials.gov/ct2/show/NCT01879553
Conditions:Human InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT01209780
Conditions:Seasonal InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT02062281
Conditions:Pneumococcal Infection|InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT01070290
Conditions:Gastric CancerLink: https://clinicaltrials.gov/ct2/show/NCT01701752
Conditions:Influenza ALink: https://clinicaltrials.gov/ct2/show/NCT01014806
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT00988741
Conditions:Unresectable Hepatocellular CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT00777309
Conditions:Non Small Cell Lung CancerLink: https://clinicaltrials.gov/ct2/show/NCT00558207
Conditions:Pancreatic NeoplasmsLink: https://clinicaltrials.gov/ct2/show/NCT00557609
Conditions:Renal Cell Carcinoma (RCC)|Alveolar Soft Part Sarcoma (ASPS)|Clear Cell Sarcoma (CCS)Link: https://clinicaltrials.gov/ct2/show/NCT00609921
Conditions:CancerLink: https://clinicaltrials.gov/ct2/show/NCT01010737
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT00612209
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
Conditions:InfluenzaLink: https://clinicaltrials.gov/ct2/show/NCT00302172
Conditions:Cancer|TumorLink: https://clinicaltrials.gov/ct2/show/NCT00658554
Conditions:HealthyLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2009-016025-34
Condition:Treatment for metastatic colorectal cancer (CRC) in combination with irinotecan and cetuximab after failure of front-line systemic therapy in subjects with wild-type KRAS alleles.Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2009-015400-26
Condition:Germ cell tumors (GCT) including testicular and non-central nervous system (non-CNS) extragonadal types.Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2008-007155-27
Condition:Unresectable hepatocellular carcinoma (HCC)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2009-011669-10
Condition:Microphthalmia Transcription Factor Associated Tumors:Clear cell sarcomaAlveolar soft part sarcomaTranslocation associated renal cell carcinoma (Renal cell carcinoma;MedDRA code manually entered in E.1.2)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2007-004634-17
Condition:Non-Small Cell Lung Cancer (phase 3b/4)Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2007-004622-25
Condition:Locally Advanced or Metastatic Gastric CancerLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2007-002727-32
Condition:Unresectable Locally Advanced or Metastatic Pancreatic AdenocarcinomaProducts are for research use only; We do not sell to patients
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