Adavosertib Liposomes, Formulation WD4

SKU: DLL-0005

$995.00 – $4,995.00

PEGylated liposomes containing Wee-1 kinase inhibitor adavosertib (MK1775; AZD1775), remote loaded by an ammonium sulfate gradient. The lipid composition of the liposomes is the same as Doxil. Sterile filtered and supplied ready for use in preclinical studies in rodents or in vitro. Adavosertib is a potent, ATP-competitive Wee-1 kinase inhibitor, which hinders the G2 DNA damage response checkpoint and is reported to enhance cytotoxic effects of several compounds including 5-FU and NSC 613327. For preclinical research use only.

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Product Data:

Figure 1 (Thumbnail).  Enhancement of solubility for adavosertib is shown in the representative images. Adavosertib is insoluble in aqueous media at the specified concentration (1 mg/mL). Matched concentration of adavosertib liposomes is shown after loading by ammonium sulfate gradient.

 

Figure 2. DLS analysis of Adavosertib Liposomes, Formulation WD4 (batch 10003). The average size and PDI of triplicate measurements are annotated on the representative snapshot from DLS data acquisition screen. The data are representative of a typical batch.

 

 

 

 

 

 

Details

Adavosertib is a potent, ATP-competitive Wee-1 kinase inhibitor, which hinders the G2 DNA damage response checkpoint [1, 2]. Adavosertib is reported to enhance cytotoxic effects of several compounds including 5-FU and NSC 613327 [2, 3]. Adavosertib is insoluble in water. Formulation WD4 is a liposome pre-formulated version of adavosertib which is supplied at 1.0 mg/mL adavosertib in preformed liposomes and is ready to use for in vitro or in vivo preclinical studies. Adavosertib is remote loaded by an ammonium sulfate gradient. The liposomes are PEGylated to enhance circulation time and reduce RES uptake in vivo. This product could be used alone or as a potentiating agent in combination with other bioactive compounds, depending on the mechanism of action of the companion agent. For preclinical research use only.

 

DLL-0005

PEGylated liposomes loaded with Adavosertib by ammonium sulfate gradient
Formulation No. WD4
Lipid Composition HSPC/Chol/DSPE-mPEG2000 (56.2/38.5/5.3, mol/mol)
Concentration Total Lipid 27.2 mM
Concentration Adavosertib 1.0 mg/mL
Hydration Solution 250 mM Ammonium Sulfate, pH 5.5
External Solution Normal Saline (154 mM NaCl, pH 5.5)
Liposome Avg. Size 70-120 nm
 

Bioactive Compound Details

 
Encapsulated Compound Adavosertib
Alias(es) AZD-1775; MK-1775
CAS No. 955365-80-7
Target Wee1 kinase
Signaling Pathway DNA damage response
CAS No. AZD-1775; MK-1775
Description Adavosertib is a potent Wee1 inhibitor with an IC50 of 5.2 nM.

 

 

 

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Additional Information

Additional Information

Liquid, suspension
2 °C to 8 °C (do not freeze)
Shelf Life* 6 months
HSPC: L-α-phosphatidylcholine, hydrogenated (Soy); Chol : Cholesterol; DSPE-mPEG2000: 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000]

*When maintained under the specified storage conditions.