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DCC-2618

Cat. No. M20635
DCC-2618 Structure
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Biological Activity

DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of KIT and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth.

Chemical Information
Molecular Weight 489.47
Formula C26H21F2N5O3
CAS Number 1225278-16-9
Solubility (25°C) DMSO 97 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. Ripretinib

[2] Andreas Reiter, et al. Blood. New developments in diagnosis, prognostication, and treatment of advanced systemic mastocytosis

[3] Bryan D Smith, et al. Cancer Cell. Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants

[4] Mathias Schneeweiss, et al. Haematologica. The KIT and PDGFRA switch-control inhibitor DCC-2618 blocks growth and survival of multiple neoplastic cell types in advanced mastocytosis

[5] No authors listed. Cancer Discov. BLU-285, DCC-2618 Show Activity against GIST

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