Quizartinib, Free BaseAn Flt-3/Flk-2 inhibitor

Quizartinib, Free Base (CAS 950769-58-1)

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Synonym: AC-220
Application: An Flt-3/Flk-2 inhibitor
CAS Number: 950769-58-1
Purity: ≥98%
Molecular Weight: 560.67
Molecular Formula: C29H32N6O4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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Quizartinib, Free Base, is an fms-related tyrosine kinase 3 (FLT3) receptor tyrosine kinase inhibitor. In binding assays, quizartinib has demonstrated a high affinity for FLT3 (Kd = 1.6 nM). in vitro assays examining FLT3 internal tandem duplicate mutations and wild-type FLT3 demonstrate the ability of quizartinib to inhibit FLT3 autophosphorylation (IC50 = 1.1 nM for FLT3-ITD and 4.2 nM for wt FLT3). Quizartinib, Free Base, has also been shown to inhibit the growth of human leukemia cell line MV4-11 (IC50 = 0.56 nM) and A375 cells (IC50 > 10,000 nM).


References

1. Zarrinkar, Patrick P., et al., 2009. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood. 114(14): 2984-92. PMID: 19654408
2. Pratz, Keith W., et al., 2010. FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML. Blood. 115(7): 1425-32. PMID: 20007803
3. Sato, Takashi., et al., 2011. FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo. Blood. 117(12): 3286-93. PMID: 21263155

Physical State :
Solid
Storage :
Store at -20° C
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
24889392
SMILES :
CC(C)(C)C1=CC(=NO1)NC(=O)NC2=CC=C(C=C2)C3=CN4C5=C(C=C(C=C5)OCCN6CCOCC6)SC4=N3

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Certificate of Analysis

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