WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206497
CAS#: 1442472-39-0 (free base)
Description: Ripretinib, also known as DCC-2618, is a potent, orally active and selective KIT/PDGFR inhibitor with potential antineoplastic activity. 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. In May 2020, FDA Approves Qinlock (ripretinib) for the Treatment of Fourth-Line Gastrointestinal Stromal Tumor
MedKoo Cat#: 206497
Name: Ripretinib free base
CAS#: 1442472-39-0 (free base)
Chemical Formula: C24H21BrFN5O2
Exact Mass: 509.0863
Molecular Weight: 510.3674
Elemental Analysis: C, 56.48; H, 4.15; Br, 15.66; F, 3.72; N, 13.72; O, 6.27
Related CAS #: 1442472-39-0 (free base) Ripretinib HCl 1225278-16-9 (wrong structure for DCC-2618)
Synonym: DCC-2618; DCC 2618; DCC2618; DP 2618; DP-2618; DP2618; Ripretinib;
IUPAC/Chemical Name: 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
InChi Key: CEFJVGZHQAGLHS-UHFFFAOYSA-N
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)
SMILES Code: O=C(NC1=CC(C2=CC3=C(C=C(NC)N=C3)N(CC)C2=O)=C(Br)C=C1F)NC4=CC=CC=C4
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 510.3674 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Baird JH, Gotlib J. Clinical Validation of KIT Inhibition in Advanced Systemic
Mastocytosis. Curr Hematol Malig Rep. 2018 Oct;13(5):407-416. doi:
10.1007/s11899-018-0469-3. Review. PubMed PMID: 30155614.
2: Schneeweiss M, Peter B, Bibi S, Eisenwort G, Smiljkovic D, Blatt K, Jawhar M,
Berger D, Stefanzl G, Herndlhofer S, Greiner G, Hoermann G, Hadzijusufovic E,
Gleixner KV, Bettelheim P, Geissler K, Sperr WR, Reiter A, Arock M, Valent P. 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. doi: 10.3324/haematol.2017.179895. Epub 2018 Feb 8. PubMed
PMID: 29439183; PubMed Central PMCID: PMC5927976.
3: BLU-285, DCC-2618 Show Activity against GIST. Cancer Discov. 2017
Feb;7(2):121-122. doi: 10.1158/2159-8290.CD-NB2016-165. Epub 2017 Jan 11. PubMed
PMID: 28077435.
Note: Many vendors listed wrong structure with CAS#1225278-16-9
