Quizartinib (AC220)
Cat. No.: DC5197
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Chemical Structure
950769-58-1
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Field of application
Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Phase 1/2.
| Cas No.: |
950769-58-1 |
| Chemical Name: |
1-(5-(tert-butyl)isoxazol-3-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea |
| Synonyms: |
AC220; AC 220; AC-220; AC010220; AC-010220; AC 010220; AC010220; Quizartinib. |
| SMILES: |
N(C1C=C(C(C)(C)C)ON=1)C(NC1=CC=C(C2=CN3C4=CC=C(OCCN5CCOCC5)C=C4SC3=N2)C=C1)=O |
| Formula: |
C29H32N6O4S |
| M.Wt: |
560.673 |
| Sotrage: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
Quizartinib (AC220) is a potent Flt3 tyrosine kinase inhibitor with a Kd of 1.6±0.7 nM. |
| In Vivo: |
Quizartinib (AC220) inhibits FLT3 activity in vivo, significantly extends survival in a mouse model of FLT3-ITD AML at doses as low as 1 mg/kg when dosed orally once a day, eradicates tumors in a FLT3-dependent mouse xenograft model at 10 mg/kg, and potently inhibits FLT3 activity in primary patient cells. The oral bioavailability of Quizartinib, determined in rats by comparing oral and intravenous pharmacokinetics at 3 mg/kg, is approximately 40%. A single 10 mg/kg dose of Quizartinib is administered by oral gavage, and mice are killed at 2 time points after dosing, using groups of 4 animals each. Quantitation of total FLT3 and phospho-FLT3 in tumor samples revealed time-dependent inhibition of FLT3 autophosphorylation. FLT3 activity is inhibited by 90% at 2 hours, and 40% at 24 hours after administration. The extent of inhibition therefore correlated well with the expected free Quizartinib plasma levels, based on pharmacokinetic experiments[1]. |
| In Vitro: |
Quizartinib (AC220) is a novel compound expressly optimized as a FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). Quizartinib inhibits FLT3-WT and FLT3-ITD autophosphorylation with IC50 of 4.2±0.3 nM and 1.1±0.1 nM, respectively. Quizartinib inhibits MV4-11 and A375 cells with IC50 of 0.56±0.3 nM and >10 000 nM, respectively. Quizartinib inhibits FLT3 with low nanomolar potency in cellular assays and is highly selective when screened against the majority of the human protein kinome[1]. |
MSDS
COA
| LOT NO. |
DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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