Quizartinib (AC220; AC010220)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 500mg | $580 | In Stock |
| 1g | $980 | In Stock |
| 5g | $1655 | In Stock |
: Cat #: V0584 CAS #: 950769-58-1 Purity ≥ 98%
Description: Quizartinib (formerly also know as AC-220; AC-010220, brand name Vanflyta in Japan) is a novel, potent, 2nd-generation, and orally bioavailable FLT3 tyrosine kinase inhibitor for Flt3 (ITD/WT) with potential anticancer activity.
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| Molecular Weight (MW) | 560.67 |
|---|---|
| Molecular Formula | C29H32N6O4S |
| CAS No. | 950769-58-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 33.2 mg/mL (59.2 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 15% Captisol: 30 mg/mL |
| SMILES Code | O=C(NC1=CC=C(C2=CN3C(SC4=CC(OCCN5CCOCC5)=CC=C34)=N2)C=C1)NC6=NOC(C(C)(C)C)=C6 |
| Synonyms | Quizartinib; AC220 or AC010220; AC 220; AC-220; AC-010220; AC 010220; |
| Protocol | 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. |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.7836 mL | 8.9179 mL | 17.8358 mL | 35.6716 mL |
| 5mM | 0.3567 mL | 1.7836 mL | 3.5672 mL | 7.1343 mL |
| 10mM | 0.1784 mL | 0.8918 mL | 1.7836 mL | 3.5672 mL |
| 20mM | 0.0892 mL | 0.4459 mL | 0.8918 mL | 1.7836 mL |
The molarity calculator equation
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The dilution calculator equation
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
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%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.