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Ripretinib

Cat. No. M9903

All AbMole products are for research use only, cannot be used for human consumption.

Ripretinib Structure
Synonym:

DCC-2618

Size Price Availability Quantity
5mg USD 200  USD200 In stock
10mg USD 325  USD325 In stock
25mg USD 600  USD600 In stock
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Quality Control & Documentation
Biological Activity

Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFR-alpha inhibitor. Ripretinib (DCC-2618) suppresses phosphorylation of KIT and decreases the expression of phosphosphorylated (p)STAT5, pAKT and pERK1/2 in neoplastic mast cells.

Chemical Information
Molecular Weight 510.36
Formula C24H21BrFN5O2
CAS Number 1442472-39-0
Solubility (25°C) DMSO 32 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] 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

[2] Cancer Discov. BLU-285, DCC-2618 Show Activity against GIST

Related c-Kit Products
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Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.

Pexidartinib

Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively.

Motesanib

Motesanib (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret.

Masitinib mesylate

Masitinib (AB-1010) mesylate is a potent, orally bioavailable and selective inhibitor of c-Kit, IC50 of 200 nM for human recombinant c-Kit. It also inhibits PDGFRα/β, LynB with IC50 values of 540, 800 and 510 nM.

DCC-2618

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.

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Keywords: Ripretinib, DCC-2618 supplier, c-Kit, inhibitors, activators

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