Art. -Nr.: HY-112306

Ripretinib

(Synonyms: DCC-2618)

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

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). DCC-2618 exerts antineoplastic effect and induces apoptosis.

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Reinheit: 98.71%
CAS. Nr.: 1442472-39-0
Formel: C₂₄H₂₁BrFN₅O₂
Molecular Weight:510.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ripretinib Chemical Structure

CAS. Nr.: 1442472-39-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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].

IC₅₀ & Target^[1]^[2]

PDGFRA

KIT

Alle PDGFR Isoform-spezifische Produkte anzeigen :

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	8.037 μM Compound: 4; DCC-2618	Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay	[PMID: 30204441]

In Vitro

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 ROSA^{KIT 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1442472-39-0
Appearance Solid
Molecular Weight 510.36
Formel C₂₄H₂₁BrFN₅O₂
Color White to light yellow
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
Synonyms

DCC-2618
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

All Cell Proliferation/Viability AssayWB

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Journal Impact Factor

Autophagy

Kit-mediated autophagy suppression driven by a viral oncoprotein emerges as a crucial survival mechanism in Merkel cell carcinoma. [Abstract]

2025 Jul;21(7):1523-1543. PMID: 40108758

Ripretinib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jul;21(7):1523-1543. [Abstract]

Ripretinib (10^-2-10² μM; 24 h) induced apoptosis of WaGa cells.

Ripretinib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jul;21(7):1523-1543. [Abstract]

Ripretinib (0.1-20 μM; 24 h) reduced KIT phosphorylation and increased cleaved PARP levels in WaGa cells.
NPJ Precis Oncol

Clinical and preclinical insights into a novel MDM2::PDGFRA fusion in recurrent glioblastoma. [Abstract]

2025 Aug 16;9(1):289. PMID: 40819143

Ripretinib purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Aug 16;9(1):289. [Abstract]

Ripretinib (1-100 nM; 2 h) significantly inhibited PDGFRA autophosphorylation in Ba/F3 cells expressing MDM2::PDGFRA or PDGFRA D842V.

Ripretinib purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Aug 16;9(1):289. [Abstract]

Dose-response cell viability of onco-addicted Ba/F3 cells expressing MDM2::PDGFRA after treatment with Ripretinib (0.0001-10000 nM; 72 h).
Cancers (Basel)

Cabozantinib Sensitizes NSCLC Cells to Radiation by Inducing Ferroptosis via STAT3/MCL1/BECN1/SLC7A11 Axis Suppression. [Abstract]

2025 Sep 9;17(18):2950. PMID: 41008795
Analyst

Quantification of buparlisib in human liver microsomes employing an ultra-fast, sensitive UPLC-MS/MS method: in vitro and in silico metabolic stability evaluation. [Abstract]

2026 Feb 16;151(4):1058-1070. PMID: 41589698
Clin Genitourin Cancer

Targeting KIT With Antibody-Drug Conjugates in Chromophobe Renal Cell Carcinoma. [Abstract]

2025 Aug;23(4):102359. PMID: 40408838

Ripretinib purchased from MedChemExpress. Usage Cited in: Clin Genitourin Cancer. 2025 Aug;23(4):102359. [Abstract]

Ripretinib (1 μM; 120 h) decreased viability of three ChRCC cell lines (RCJ-T1, RCJ-T2, and RCJ-M).
bioRxiv

2026 Mar 25.
bioRxiv

2026 Feb 20.
bioRxiv

A Hotspot Phosphorylation Site on SHP2 Drives Oncoprotein Activation and Drug Resistance. [Abstract]

2025 Jun 16:2025.06.11.659120. PMID: 40667115

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (48.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9594 mL

9.7970 mL

19.5940 mL

5 mM

0.3919 mL

1.9594 mL

3.9188 mL

10 mM

0.1959 mL

0.9797 mL

1.9594 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (4.08 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.08 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. KIT/PDGFR Inhibitor DCC-2618.

[2]. BLU-285, DCC-2618 Show Activity against GIST. Cancer Discov. 2017 Feb;7(2):121-122. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9594 mL	9.7970 mL	19.5940 mL	48.9850 mL
	5 mM	0.3919 mL	1.9594 mL	3.9188 mL	9.7970 mL
	10 mM	0.1959 mL	0.9797 mL	1.9594 mL	4.8985 mL
	15 mM	0.1306 mL	0.6531 mL	1.3063 mL	3.2657 mL
	20 mM	0.0980 mL	0.4899 mL	0.9797 mL	2.4493 mL
	25 mM	0.0784 mL	0.3919 mL	0.7838 mL	1.9594 mL
	30 mM	0.0653 mL	0.3266 mL	0.6531 mL	1.6328 mL
	40 mM	0.0490 mL	0.2449 mL	0.4899 mL	1.2246 mL

Keywords

Ripretinib

8 Cited Publications

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Ripretinib

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Publications Citing Use of MedChemExpress (MCE) Ripretinib

Alle PDGFR Isoform-spezifische Produkte anzeigen

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ripretinib Related Classifications

HY-112306 Related Classifications