Quizartinib
| Code | Size | Price |
|---|
| SYN-1003-M100 | 100 mg | Enquire |
Quantity:
| SYN-1003-M001 | 1 mg | £115.00 |
Quantity:
| SYN-1003-M005 | 5 mg | £233.00 |
Quantity:
| SYN-1003-M010 | 10 mg | £373.00 |
Quantity:
| SYN-1003-M050 | 50 mg | £1,053.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
AC220
Appearance:
Solid.
CAS:
950769-58-1
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Hazards:
H303, H317, H333
InChi:
InChI=1S/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-16-21(8-9-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34/h4-9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36)
InChiKey:
MKGMVQKQNTXMPT-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 950769-58-1. Formula: C29H32N6O4S. MW: 560.7. 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-IAAP photolabeling of ABCG2 and ABCB1 with IC(50) values of 0.07 and 3.3µM, respectively.
Molecular Formula:
C29H32N6O4S
Molecular Weight:
560.7
Package Type:
Plastic Vial
Precautions:
P280, P301, P312, P304, P312, P302, P352, P333, P313
Product 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.
Purity:
>95%
Signal word:
Warning
Solubility Chemicals:
Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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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