Name | N-(5-tert-Butylisoxazol-3-yl)-N-{4-[7-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea |
Synonyms | CS-53 AC220 AC-220 QUIZARTINIB quizartinib (FLT3 inhibitor) 1-(5-(tert-Butyl)isoxazol-3-yl)-3-(4-(7-(2-morpholinoethoxy)-benzo[d]imidazo[2,1-b]thiazol-2-y N-(5-tert-Butylisoxazol-3-yl)-N-{4-[7-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea N-(5-tert-Butylisoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea N-[5-(1,1-Dimethylethyl)-3-isoxazolyl]-N'-[4-[7-[2-(4-morpholinyl)ethoxy]imidazo[2,1-b]benzothiazol-2-yl]phenyl]urea N-(5-tert-Butylisoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea AC-220 |
CAS | 950769-58-1 |
Molecular Formula | C29H32N6O4S |
Molar Mass | 560.67 |
Density | 1.39±0.1 g/cm3(Predicted) |
Solubility | DMSO 33.2 mg/mL; Water <0.3 mg/mL; Ethanol <0.5 mg/mL |
Appearance | White powder. |
Color | Off-white |
pKa | 12.59±0.70(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
Use | An Flt-3/Flk-2 inhibitor. |
In vitro study | AC220 is the most potent FLT3 selective inhibitor for the treatment of acute myeloid leukemia (AML). AC220 has a low nanomolar effect and specific kinase selectivity in biochemical and cellular experiments, with high selectivity for inhibition of most human protein kinases. AC220 is a novel FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). AC220 is the most potent FLT3 selective inhibitor for the treatment of acute myeloid leukemia (AML). AC220 has a low nanomolar effect and specific kinase selectivity in biochemical and cellular experiments, with high selectivity for inhibition of most human protein kinases. AC220 is a novel FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). |
In vivo study | AC220 acts on the transplanted tumor model, has good drug properties, high efficacy and tolerance. In vivo, AC220 acts on FLT3-ITD AML mouse model, inhibits FLT3 activity, significantly prolongs life span; Acts on FLT3 dependent transplanted tumor mouse model, eradicating tumor; Acts on primary cells of patients, effective inhibition of FLT3 activity. AC220 acts on the transplanted tumor model, has good drug properties, high efficacy and tolerance. In vivo, AC220 acts on FLT3-ITD AML mouse model, inhibits FLT3 activity, significantly prolongs life span; Acts on FLT3 dependent transplanted tumor mouse model, eradicating tumor; Acts on primary cells of patients, effective inhibition of FLT3 activity. |
biological activity | Quizartinib (AC220) is a second-generation FLT3 inhibitor that acts on Flt3(ITD/WT),IC50 is 1.1 nM/4.2 nM, and the selectivity of Flt3 is 10 times higher than that of KIT, PDGFRA, PDGFRB, RET, and CSF-1R. Phase 3. Quizartinib (AC220) is a second-generation FLT3 inhibitor that acts on Flt3(ITD/WT) in MV4-11 and RS4. IC50 in 11 cells is 1.1 nM/4.2 nM respectively, and the selectivity for Flt3 is 10 times higher than that for KIT,PDGFRA,PDGFRB,RET, and CSF-1R. Quizartinib (AC220) can induce apoptosis of tumor cells. Phase 3. |
in vitro study | AC220 is the most effective FLT3 selective inhibitor and can be used to treat acute myeloid leukemia (AML). AC220 has low nanomolar effect and special kinase selectivity in biochemical and cellular experiments, and has high selectivity when inhibiting most human protein kinases. AC220 is a novel FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). AC220 is the most effective FLT3 selective inhibitor and can be used to treat acute myeloid leukemia (AML). AC220 has low nanomolar effect and special kinase selectivity in biochemical and cellular experiments, and has high selectivity when inhibiting most human protein kinases. AC220 is a novel FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). |
in vivo study | AC220 acts on transplanted tumor model and has good drug properties, extremely high drug efficacy and tolerance. In vivo, AC220 acts on FLT3-ITD AML mouse model to inhibit FLT3 activity and obviously prolong life span. When acting on FLT3-dependent transplanted tumor mouse model, tumor will be eradicated. When acting on primary cells of patients, FLT3 activity is effectively inhibited. AC220 acts on the transplanted tumor model and has good drug properties, extremely high efficacy and tolerance. In vivo, AC220 acts on FLT3-ITD AML mouse model to inhibit FLT3 activity and obviously prolong life span. When acting on FLT3-dependent transplanted tumor mouse model, tumor will be eradicated. When acting on primary cells of patients, FLT3 activity is effectively inhibited. |
characteristics | AC220 is a second-generation FLT3 inhibitor and is the first candidate for clinical FLT3 inhibitors. |
target | TargetValue FLT3 (ITD) (MV4-11 cells) 1.1 nM FLT3 (WT) (RS4;11 cells) 4.2 nM |
Target | Value |
FLT3 (ITD) (MV4-11 cells) | 1.1 nM |
FLT3 (WT) (RS4;11 cells) | 4.2 nM |