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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