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| 25mg |
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| 100mg |
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Purity: ≥98%
Barasertib phosphate (also known as AZD-1152), the phosphate salt of Barasertib, is an investigational, highly selective, orally bioavailable small-molecule Aurora B inhibitor (IC50 = 0.37 nM in a cell-free assay) with anticancer activity. It is a pro-drug of barasertib-hQPA that is dihydrogen phosphate. Barasertib exhibits inhibitory effects against a variety of aurora kinases, such as the FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutation, as well as aurora A kinase (AKB), aurora B kinase (ABK), and aurora C kinase (ACK), with inhibition constants (Ki) of 1369 nM, 0.36 nM, and 17.0 nM, respectively.
| Targets |
Aurora B (IC50 = 10.37 nM)
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| ln Vitro |
Barasertib-HQPA (3 μM, 3 hours) considerably reduces the expression of histone H3 phosphorylation in newly isolated leukemia cells[1].
Barasertib-hydroxyquinazoline pyrazol anilide (HQPA)] is quickly changed in plasma to the active form of barasertib-HQPA[2]. Barasertib-HQPA is employed in the in vitro research[3]. Barasertib-HQPA causes a polyploid population to emerge along with a noticeable anti-propliferative effect that, in most cases, results in apoptosis[4]. |
| ln Vivo |
Barasertib (AZD1152, 25 mg/kg) significantly inhibits the weight gain and growth of tumors treated with AZD1152[1].
Barasertib (AZD1152, 5 mg/kg) improves vincristine's or daunorubicin's capacity to stop human MOLM13 leukemic xenografts from proliferating[1]. Barasertib (AZD1152, (10-150 mg/kg/d)significantly reduced the growth of xenografts of human colon, lung, and hematologic tumors (mean tumor growth inhibition range, 55% to z100%; P < 0.05)[2]. |
| Animal Protocol |
Female immune-deficient BALB/c nude mice (MOLM13 cells injected)[1].
5 or 25 mg/kg. Intraperitoneal injection 4 times a week or every another day. |
| References |
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| Molecular Formula |
C26H31FN7O6P
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|---|---|---|
| Molecular Weight |
587.54
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| Exact Mass |
587.21
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| Elemental Analysis |
C, 53.15; H, 5.32; F, 3.23; N, 16.69; O, 16.34; P, 5.2 7
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| CAS # |
722543-31-9
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| Related CAS # |
Barasertib-HQPA;722544-51-6
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| Appearance |
Solid powder
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| SMILES |
CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCOP(=O)(O)O
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| InChi Key |
GBJVVSCPOBPEIT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H31FN7O6P/c1-2-34(10-12-40-41(36,37)38)9-4-11-39-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(35)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17H,2,4,9-12,15H2,1H3,(H,30,35)(H2,36,37,38)(H2,28,29,31,32,33)
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| Chemical Name |
2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethyl dihydrogen phosphate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.26 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.26 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (3.69 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.17 mg/mL (3.69 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 2.17 mg/mL (3.69 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: 2% DMSO+40% PEG 300+2% Tween 80+ddH2O: 7mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7020 mL | 8.5101 mL | 17.0201 mL | |
| 5 mM | 0.3404 mL | 1.7020 mL | 3.4040 mL | |
| 10 mM | 0.1702 mL | 0.8510 mL | 1.7020 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
Summary of the number of progenitor colonies formed/ml of methylcellulose medium supplemented with differing concentrations of AZD1152 ().Cancer Res.2009 May 15;69(10):4150-8. |
The induction of polyploidy by AZD1152-HQPA in HL-60 and THP-1 cells.Cancer Res.2009 May 15;69(10):4150-8. |
AZD1152-HQPA inhibited cell proliferation, induced cytotoxicity and inhibited phosphorylation of histone H3 (ser10) in AML cell lines.Cancer Res.2009 May 15;69(10):4150-8. |
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