Ripretinib (Synonyms: DCC-2618) |
Catalog No.GC37538
One-Click Copy Product Info
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Le riprétinib (DCC-2618) est un inhibiteur de contrÔle de commutation KIT et PDGFRA biodisponible par voie orale. Le riprétinib (DCC-2618) cible et se lie À la fois aux formes de type sauvage et mutantes de KIT et de PDGFRA spécifiquement au niveau de leurs sites de liaison de poche de commutation, empêchant ainsi le passage de conformations inactives À actives de ces kinases et inactivant leurs formes de type sauvage et mutantes . Le riprétinib (DCC-2618) inhibe également plusieurs autres cibles kinases, telles que FLT3 et KDR (ou VEGFR-2). Le DCC-2618 exerce un effet antinéoplasique et induit l'apoptose.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1442472-39-0
Sample solution is provided at 25 µL, 10mM.
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Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2)[1][2]. DCC-2618 exerts antineoplastic effect and induces apoptosis[3].
Ripretinib (DCC-2618) suppresses phosphorylation of KIT and decreases the expression of phosphosphorylated (p)STAT5, pAKT and pERK1/2 in neoplastic mast cells. Ripretinib inhibits the growth of ROSAKIT K509I cells with an IC50 of 34 ± 10 nM, and also induces apoptosis in these cells. Ripretinib (0.1-1.0 μM) inhibits IgE-dependent histamine release from basophils and spontaneous tryptase release from neoplastic mast cells, and also counteracts growth and survival of leukemic monocytes and blast cells at 0.01-5 μM[2].Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, shows cytotoxic activity against gastrointestinal stromal tumors[4].
References:
[1]. Schneeweiss M, et al. The KIT and PDGFRA switch-control inhibitor DCC-2618 blocks growth and survival of multiple neoplastic cell types in advanced mastocytosis. Haematologica. 2018 May;103(5):799-809.
[2]. KIT/PDGFR Inhibitor DCC-2618.
[3]. Schneeweiss M, et al. The KIT and PDGFRA switch-control inhibitor DCC-2618 blocks growth and survival of multiple neoplastic cell types in advanced mastocytosis. Haematologica. 2018 May;103(5):799-809.
[4]. BLU-285, DCC-2618 Show Activity against GIST. Cancer Discov. 2017 Feb;7(2):121-122.
| Cas No. | 1442472-39-0 | SDF | |
| Synonymes | DCC-2618 | ||
| Canonical SMILES | O=C(NC1=CC(C2=CC3=C(C=C(NC)N=C3)N(CC)C2=O)=C(Br)C=C1F)NC4=CC=CC=C4 | ||
| Formula | C24H21BrFN5O2 | M.Wt | 510.36 |
| Solubility | DMSO: 45 mg/mL (88.17 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9594 mL | 9.797 mL | 19.594 mL |
| 5 mM | 391.9 μL | 1.9594 mL | 3.9188 mL |
| 10 mM | 195.9 μL | 979.7 μL | 1.9594 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)