| Size | Price | Stock | Qty |
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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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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
| Targets |
PDGFR; WT KIT (IC50 = 4 nM); D816H KIT (IC50 = 5 nM); V654A KIT (IC50 = 8 nM); D816V KIT (IC50 = 14 nM)
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| ln Vitro |
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| ln Vivo |
In the GIST T1 xenograft model, DCC-2618 administration at 50 mg/kg results in an ED90 for KIT phosphorylation inhibition, which corresponds to an EC90 concentration of roughly 470 ng/mL. This oral dose causes nearly total tumor stasis when taken twice a day. In a KIT exon 17 N822K AML xenograft model and a patient-derived xenograft (PDX) GIST expressing KIT exon 11 delW557K558/exon 17 Y823D, this dosage of DCC-2618 results in tumor regressions[1]. DCC-2618 inhibits PDGFRA- and KIT-driven tumor growth in xenograft studies, including KIT exon 17 mutants present in AML (N822K), GIST (Y823D), and mastocytosis (D816V) models[3].
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| Enzyme Assay |
In order to assess KIT and BTK signaling, ROSAKIT WT, ROSAKIT D816V, HMC-1.1, and HMC-1.2 cells were incubated for 4 hours at 37°C in either control medium or DCC-2618 (0.5–5 μM). Western blotting was done essentially according to other instructions. In order to assess the downstream signaling pathways of KIT, HMC-1.1, HMC-1.2, ROSAKIT WT, and ROSAKIT D816V cells were initially pre-cultured for an entire night in Iscove-modified Dulbecco medium that was devoid of stem cell factor and fetal calf serum. Then, for 90 minutes at 37°C, DCC-2618 (0.001–10 μM) was applied to 106 cells from each line. Following the course of treatment, ROSAKIT WT cells were stimulated for 10 minutes at room temperature using 10% of the supernatants of Chinese hamster ovary cells transfected with the murine scf (kl) gene (CHO-KL). Western blotting was then carried out essentially in the same manner as previously mentioned.
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| Cell Assay |
In order to assess KIT and BTK signaling, HMC-1.1, HMC-1.2, ROSA (KIT WT), and ROSA (KIT D816V) cells are incubated for 4 hours at 37°C in either control medium or DCC-2618 (0.5–5 μM). One method used is western blotting.
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| Animal Protocol |
xenograft models (mice)
100 mg/kg/day or 25 mg/kg/day or 50 mg/kg BID oral |
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| References |
| Molecular Formula |
C24H21BRFN5O2
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|---|---|---|
| Molecular Weight |
510.37
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| Exact Mass |
509.09
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| Elemental Analysis |
C, 56.48; H, 4.15; Br, 15.66; F, 3.72; N, 13.72; O, 6.27
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| CAS # |
1442472-39-0
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| Related CAS # |
1442472-39-0;Ripretinib HCl 1225278-16-9 (wrong structure for DCC-2618);
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| Appearance |
White to off-white solid powder
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| SMILES |
CCN1C2=CC(=NC=C2C=C(C1=O)C3=CC(=C(C=C3Br)F)NC(=O)NC4=CC=CC=C4)NC
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| InChi Key |
CEFJVGZHQAGLHS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H21BrFN5O2/c1-3-31-21-12-22(27-2)28-13-14(21)9-17(23(31)32)16-10-20(19(26)11-18(16)25)30-24(33)29-15-7-5-4-6-8-15/h4-13H,3H2,1-2H3,(H,27,28)(H2,29,30,33)
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| Chemical Name |
1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl]-2-fluorophenyl]-3-phenylurea
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
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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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9594 mL | 9.7968 mL | 19.5936 mL | |
| 5 mM | 0.3919 mL | 1.9594 mL | 3.9187 mL | |
| 10 mM | 0.1959 mL | 0.9797 mL | 1.9594 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 |
| NCT03673501 | Active Recruiting |
Drug: DCC-2618 Tablets Drug: Sunitinib |
Gastrointestinal Stromal Tumors | Deciphera Pharmaceuticals LLC | February 11, 2019 | Phase 3 |
| NCT05697107 | Active Recruiting |
Drug: Ripretinib Oral Tablet | Gastrointestinal Stromal Tumors | Peking University | May 20, 2021 | |
| NCT05132738 | Recruiting | Drug: Ripretinib treatment | Gastrointestinal Stromal Tumors | RenJi Hospital | August 1, 2021 | Not Applicable |
| NCT05734105 | Recruiting | Drug: Ripretinib Drug: Sunitinib |
GIST | Deciphera Pharmaceuticals LLC | November 2023 | Phase 3 |
| NCT05957367 | Recruiting | Drug: Ripretinib Drug: DCC-3116 |
GIST Colorectal Cancer |
Deciphera Pharmaceuticals LLC | September 28, 2023 | Phase 1 Phase 2 |
DCC-2618 and its active metabolite DP-5439 inhibit proliferation of neoplastic mast cells.Haematologica.2018 May;103(5):799-809. |
DCC-2618 inhibits phosphorylation of KIT and other targets in neoplastic mast cells.Haematologica.2018 May;103(5):799-809. |
Effects of DCC-2618 on anti-IgE-induced histamine release from normal basophils.Haematologica.2018 May;103(5):799-809. |
DCC-2618 and DP-5439 induce apoptosis in neoplastic mast cells.Haematologica.2018 May;103(5):799-809. |
Effects of DCC-2618 and DP-5439 on proliferation and survival of acute myeloid leukemia (AML) and chronic myelomonocytic leukemia (CMML).Haematologica.2018 May;103(5):799-809. |
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