[CAS NO. 1442472-39-0] Ripretinib
PRODUCTS SPECIFICATIONS [1442472-39-0]
DESCRIPTION [1442472-39-0]
Overview
| MDL | MFCD31657437 |
|---|---|
| Molecular Weight | 510.36 |
| Molecular Formula | C24H21BrFN5O2 |
| 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 |
Summary
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
|
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 ROSA
KIT K509I
cells with an IC
50
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT05080621 | Deciphera Pharmaceuticals LLC |
Gastrointestinal Stromal Tumors
|
November 2021 | Phase 1|Phase 2 |
| NCT03353753 | Deciphera Pharmaceuticals LLC |
Gastrointestinal Stromal Tumors
|
February 27, 2018 | Phase 3 |
| NCT04282980 | Zai Lab (Shanghai) Co., Ltd.|Zai Lab (Hong Kong), Ltd. |
Gastrointestinal Stromal Tumors
|
April 23, 2020 | Phase 2 |
| NCT04633122 | Zai Lab (Shanghai) Co., Ltd.|Zai Lab (Hong Kong), Ltd. |
Gastrointestinal Stromal Tumor(GIST)
|
November 25, 2020 | Phase 2 |
| NCT04148092 | Deciphera Pharmaceuticals LLC |
GIST - Gastrointestinal Stromal Tumor
|
||
| NCT04530981 | Deciphera Pharmaceuticals LLC |
GIST - Gastrointestinal Stromal Tumor
|
September 22, 2021 | Phase 1 |
| NCT02571036 | Deciphera Pharmaceuticals LLC |
Gastrointestinal Stromal Tumors|Advanced Systemic Mastocytosis|Advanced Cancers
|
October 2015 | Phase 1 |
| NCT03673501 | Deciphera Pharmaceuticals LLC |
Gastrointestinal Stromal Tumors
|
February 11, 2019 | Phase 3 |
| NCT05132738 | RenJi Hospital |
Gastrointestinal Stromal Tumors
|
August 1, 2021 | Not Applicable |
Appearance
Solid
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
DMSO : 25 mg/mL ( 48.99 mM ; Need ultrasonic)
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 |
References
- [1] KIT/PDGFR Inhibitor DCC-2618.
- [2] BLU-285, DCC-2618 Show Activity against GIST. Cancer Discov. 2017 Feb;7(2):121-122.
- [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.
