Size | Price | Stock | Qty |
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5mg |
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10mg |
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Other Sizes |
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Targets |
CDK9/CycT1 13 nM (IC50) CDK9/CycT1(h) 6 nM (IC50) CDK3/CycE(h) 890 nM (IC50) CDK2/CycE(h) 1000 nM (IC50) CDK1/CycB(h) 1100 nM (IC50) CDK5/p35(h) 1600 nM (IC50)
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ln Vitro |
Positive transcription elongation factor b (PTEFb) is one of four cyclin partners—cyclin T1, cyclin K, cyclin T2a, or cyclin T2b—and a heterodimer of CDK9. Strong antiproliferative action against HeLa cells (IC50=920 nM) and MOLM-13 cells (IC50=310 nM) is demonstrated by atuveciclib (BAY-1143572)[1].
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ln Vivo |
Atuveciclib (BAY-1143572) has strong potency and good anticancer activity in in vivo efficacy trials conducted in the MOLM-13 xenograft model in mice. Treatment-to-control (T/C) ratios of 0.64 and 0.49, respectively, (p<0.001), representing dose-dependent antitumor effectiveness, are obtained with daily administration of Atuveciclib (BAY-1143572) at 6.25 or 12.5 mg/kg. In an additional trial, antitumor effectiveness with a T/C ratio of 0.41 and 0.31, respectively, is noted at a higher daily dose of 20 or 25 mg/kg Atuveciclib (BAY-1143572) (p<0.001). The highest amount that naked mice can withstand is 25 mg/kg given once a day. Additionally, T/C ratios of 0.33 and 0.20 (p<0.001) are obtained with Atuveciclib (BAY-1143572) when given at 25 or 35 mg/kg, three days on and two days off. Less than 10% mean body weight loss over the course of the trial indicates that atuveciclib (BAY-1143572) treatment is well-tolerated. Atuveciclib (BAY-1143572) exhibits low blood clearance (CLb 1.1 L/kg per hour) in an in vivo pharmacokinetic investigation in rats[1].
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References |
[1]. Lücking U, et al. Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer. ChemMedChem. 2017 Nov 8;12(21):1776-1793
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Molecular Formula |
C18H18FN5O2S
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Molecular Weight |
387.43
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CAS # |
2923012-24-0
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Related CAS # |
Atuveciclib Racemate;1414943-88-6;Atuveciclib S-Enantiomer;2250279-81-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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 |
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) |
DMSO : ≥ 128.5 mg/mL (331.67 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5811 mL | 12.9056 mL | 25.8111 mL | |
5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL | |
10 mM | 0.2581 mL | 1.2906 mL | 2.5811 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.