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SynKinase
Quizartinib
CHF 0.00
In stock
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SYN-1003-M100100 mgINQ
| Product Details | |
|---|---|
| Synonyms | AC220 |
| Product Type | Chemical |
| Properties | |
| Formula | C29H32N6O4S |
| MW | 560.7 |
| CAS | 950769-58-1 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: PDGFR | Kinase Group: RTK | Substrate: Tyrosine Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
| InChi Key | MKGMVQKQNTXMPT-UHFFFAOYSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
Quizartinib (AC220) is a second-generation FLT3 inhibitor that has shown promising activity in AML in Phase II clinical trials. It inhibits mutant and wild-type FLT3 in vivo at 0.1 and 0.5µM, respectively, and has shown favorable activity and tolerability in phase I and II trials in acute myeloid leukemia, with QT prolongation as the dose-limiting toxicity. Recently, AC220 has also been shown to be an effective inhibitor of ATP-binding cassette (ABC) proteins ABCB1 (P-glycoprotein) and ABCG2 (breast cancer resistance protein). Quizartinib inhibited transport of fluorescent ABCG2 and ABCB1 substrates in ABCG2- and ABCB1-overexpressing cells in a concentration-dependent manner, from 0.1 to 5µM and from 0.5 to 10µM, respectively, and inhibited [125I]-IAAP photolabeling of ABCG2 and ABCB1 with IC(50) values of 0.07 and 3.3µM, respectively.
Product References
- AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML): P.P. Zarrinkar, et al.; Blood 114, 2984 (2009)
- 3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3): J.T. Hsu, et al.; Bioorg. Med. Chem. Lett. 22, 4654 (2012)
- Combating drug resistance in acute myeloid leukaemia by drug rotations: the effects of quizartinib and pexidartinib: J. Yang, et al.; Cancer Cell Int. 21, 198 (2021)
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