An inhibitor of FLT3
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Quizartinib

Item No. 17986

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-(1,1-dimethylethyl)-3-isoxazolyl]-N'-[4-[7-[2-(4-morpholinyl)ethoxy]imidazo[2,1-b]benzothiazol-2-yl]phenyl]-urea
CAS Number
950769-58-1
Synonyms
  • AC220
Molecular Formula
C29H32N6O4S
Formula Weight
560.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 30 mg/mlEthanol: 0.25 mg/ml
λmax
295 nm
SMILES
O=C(NC1=NOC(C(C)(C)C)=C1)NC2=CC=C(C3=CN4C(SC5=C4C=CC(OCCN6CCOCC6)=C5)=N3)C=C2
InChi Code
InChI=1S/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(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)
InChi Key
CVWXJKQAOSCOAB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $32

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    1 mg

    $48

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    5 mg

    $63

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    10 mg

    $94

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    Product Description

    Quizartinib is an inhibitor of FMS-related tyrosine kinase 3 (FLT3; Kd = 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.1,2 It inhibits the proliferation of the human leukemia cell line MV4-11, which harbors a homozygous FLT3-ITD mutation, with an IC50 value of 0.56 nM.1 At 1 mg/kg/day, quizartinib has been shown to extend survival in a mouse model of FLT3-ITD acute myeloid leukemia and to eradicate tumors in an FLT3-dependent mouse xenograft model at 10 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chao, Q., Sprankle, K.G., Grotzfeld, R.M., et al. Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. J. Med. Chem. 52(23), 7808-7816 (2009).

    2. Zarrinkar, P.P., Gunawardane, R.N., Cramer, M.D., et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 114(14), 2984-2992 (2009).