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AC220 (Quizartinib) | FLT3 inhibitor

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Price:
$159.00
Catalog #:
C2222-2s
Quantity:


Product Description

AC220 (Quizartinib) is an orally-available, imidazobenzothiazole-based inhibitor of Flt3, with an in vitro Kd of 2 nM. In vitro cell studies show that AC220 has a IC50 of 0.5 nM for MV-411 cells. [1] In a variety of leukemic cell lines, AC220 inhibited Flt3 phosphorylation of MV4-11, MOLM-14, SEM-K2, and RS4-11 at IC50s of 1, 2, 4, and 4 nM, respectively. Furthermore, inhibition of cell proliferation on these same lines were measured as 0.3, 0.1, 0.4, and >10000 nM, respectively. [2]

In a KinomeScan panel of 402 kinases, AC220 has a high degree of specificity toward Flt3 with only mild inhibition of closely related RTKs such as KIT, PDGFR, RET, VEGFR2. [3]

Ina Flt3-ITD acute myeloid leukemia mouse model, AC220 was shown to extend significantly the survival at 1 mg/kg QD dosing, and eradicates tumors in a Flt3-dependent mouse xenograft model at 10 mg/kg. [3]


Technical information:

Chemical Formula:   C29H32N6O4S
CAS #:   950769-58-1
Molecular Weight:   560.67
Purity:   > 98%
Appearance:   White solid
Chemical Name:   Urea, N-[5-(1,1-dimethylethyl)-3-isoxazolyl]-N'-[4-[7-[2-(4-morpholinyl)ethoxy]imidazo[2,1-b]benzothiazol-2-yl]phenyl]-
Solubility:   Up to 100mM in DMSO
Synonyms:   AC-220, AC220, Quizartinib

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Belli et al., AC220, a uniquely potent and selective FLT3 inhibitor, enhances the cytotoxiceffects of chemotherapeutic agents in cell culture and in mouse tumor xenografts. Ambit Biosciences ASH Poster, 2009, Abstract 2052.
2. Gunawardane et al., INHIBITION OF FLT3 SIGNALING BOTH IN VITRO AND IN VIVO BY AC220, A SECOND GENERATION POTENT AND SELECTIVE FLT3 INHIBITOR. Ambit Biosciences AACR Poster, 2010, Abstract 3619.
3. Zarrinkar et al., AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 2009, 114(14), 2984-2992. Pubmed ID: 19654408

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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