1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. c-Kit
    PDGFR
    FLT3
    VEGFR
    Apoptosis
  3. Ripretinib

Ripretinib (Synonyms: DCC-2618)

Cat. No.: HY-112306 Purity: 99.46%
Handling Instructions

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.

For research use only. We do not sell to patients.

Ripretinib Chemical Structure

Ripretinib Chemical Structure

CAS No. : 1442472-39-0

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Description

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

 

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 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].

Clinical Trial
Molecular Weight

510.36

Formula

C₂₄H₂₁BrFN₅O₂

CAS No.

1442472-39-0

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 45 mg/mL (88.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 1.

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

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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.46%

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Keywords:

RipretinibDCC-2618DCC2618DCC 2618c-KitPDGFRFLT3VEGFRApoptosisSCFRCD117Platelet-derived growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Vascular endothelial growth factor receptorInhibitorinhibitorinhibit

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Ripretinib
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HY-112306
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