| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
MEK (IC50 = 160 nM); BRAF V600E (IC50 = 8.2 nM); Braf (IC50 = 190 nM); CRAF (IC50 = 56 nM)
|
|---|---|
| References |
|
| Additional Infomation |
RAMP-201 (NCT04625270) was an open-label, multicenter trial that enrolled 57 adult patients with measurable KRAS-mutant recurrent low-grade serous ovarian cancer (LGSOC) and evaluated its efficacy. Patients had to have received at least one prior systemic therapy, including platinum-based chemotherapy. KRAS mutation status was determined by prospective local testing of tumor tissue. Patients received avatinib 3.2 mg orally twice weekly (days 1 and 4) and fadatinib 200 mg orally twice daily, both administered for the first 3 weeks of each 4-week cycle until disease progression or intolerable toxicity. The primary efficacy endpoint was overall response rate (ORR), assessed by a blinded independent review committee according to RECIST v1.1. The other efficacy endpoint was duration of response (DOR). The confirmed objective response rate (ORR) was 44% (95% CI: 31, 58), and the duration of response (DOR) ranged from 3.3 months to 31.1 months. The most common adverse reactions (≥25%) included abnormal laboratory findings, elevated creatine phosphokinase, nausea, fatigue, elevated aspartate aminotransferase, rash, diarrhea, musculoskeletal pain, edema, decreased hemoglobin, elevated alanine aminotransferase, vomiting, elevated bilirubin, elevated triglycerides, decreased lymphocyte count, abdominal pain, dyspepsia, acneiform dermatitis, vitreoretinal disease, elevated alkaline phosphatase, stomatitis, pruritus, visual disturbances, decreased platelet count, constipation, dry skin, dyspnea, cough, urinary tract infection, and decreased neutrophil count. The recommended dose of avatinib is 3.2 mg (4 0.8 mg capsules) orally twice weekly (days 1 and 4) for 3 weeks, until disease progression or intolerable toxicity. The recommended dose of defatinib is 200 mg (1 tablet) orally twice daily for 3 weeks, until disease progression or intolerable toxicity occurs.
|
| Molecular Formula |
C21H18FKN5O5S
|
|---|---|
| Molecular Weight |
510.56
|
| Exact Mass |
509.0571
|
| CAS # |
946128-90-1
|
| Related CAS # |
946128-88-7; 946128-90-1
|
| PubChem CID |
51030988
|
| Appearance |
Typically exists as solids at room temperature
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
34
|
| Complexity |
851
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(C(=O)OC2=C1C=CC(=C2)OC3=NC=CC=N3)CC4=C(C(=NC=C4)[N-]S(=O)(=O)NC)F.[K+]
|
| InChi Key |
KYKJFDDJHVJFIF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H17FN5O5S.K/c1-12-15-5-4-14(31-21-25-7-3-8-26-21)11-17(15)32-20(28)16(12)10-13-6-9-24-19(18(13)22)27-33(29,30)23-2;/h3-9,11,23H,10H2,1-2H3;/q-1;+1
|
| Chemical Name |
potassium [3-fluoro-4-[(4-methyl-2-oxo-7-pyrimidin-2-yloxychromen-3-yl)methyl]-2-pyridinyl]-(methylsulfamoyl)azanide
|
| Synonyms |
Ro 5126766 potassium;
Avutometinib potassium; VS-6766 potassium; RO5126766 potassium; RO-5126766 potassium; ...; 946128-90-1; CH5126766 potassium
|
| 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 | 1.9586 mL | 9.7932 mL | 19.5863 mL | |
| 5 mM | 0.3917 mL | 1.9586 mL | 3.9173 mL | |
| 10 mM | 0.1959 mL | 0.9793 mL | 1.9586 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03681483 | Active Recruiting |
Drug: RO5126766 | Advanced Non-small Cell Lung Cancer |
Memorial Sloan Kettering Cancer Center |
October 31, 2018 | Early Phase 1 |
| NCT03875820 | Active Recruiting |
Drug: VS-6766 Drug: Defactinib |
NSCLC Pancreatic Cancer |
Institute of Cancer Research, United Kingdom |
December 12, 2017 | Phase 1 |
| NCT00773526 | Completed | Drug: RO5126766 | Neoplasms | Hoffmann-La Roche | November 2008 | Phase 1 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
