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| 5mg |
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| 10mg |
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| Targets |
CDK1[1]
Avotaciclib hydrochloride targets cyclin-dependent kinase 1 (CDK1), a serine/threonine kinase that plays a critical role in cell cycle regulation, particularly the G2/M phase transition. By inhibiting CDK1 activity, the compound disrupts normal cell cycle progression. CDK1 is often abnormally and strongly expressed in certain cancers, including pancreatic cancer and lung cancer, making it a relevant therapeutic target. |
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| ln Vitro |
In vitro, Avotaciclib hydrochloride inhibits cell viability and promotes apoptosis in radiotherapy-resistant non-small cell lung cancer cell lines (including H1437R, H1568R, H1703R, and H1869R) with EC50 values of 0.918, 0.580, 0.735, and 0.662 microM, respectively. The effect is enhanced when combined with the checkpoint kinase 2 inhibitor PV-1019. The compound is tested at concentrations ranging from 0 to 64 microM for 48 hours.
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| ln Vivo |
In vivo, Avotaciclib hydrochloride is an orally active CDK1 inhibitor that inhibits tumor cell proliferation and induces apoptosis. It is being researched for use in locally advanced or metastatic pancreatic cancer and lung cancer models. While specific in vivo efficacy data (e.g., tumor xenograft studies) are not detailed in product datasheets, its oral bioavailability and antitumor activity have been demonstrated in preclinical cancer models.
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| Enzyme Assay |
For Avotaciclib hydrochloride, CDK1 binding/inhibition is measured using cell-free kinase assays with purified recombinant CDK1/cyclin B complexes. Serial dilutions of the compound are incubated with the kinase, its substrate (e.g., histone H1), and ATP. The remaining kinase activity is quantified by measuring phosphorylated product using methods such as ADP-Glo or radioactivity-based detection (e.g., filter-binding of 33P-ATP).
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| Cell Assay |
For Avotaciclib hydrochloride, radiotherapy-resistant non-small cell lung cancer cells (H1437R, H1568R, H1703R, H1869R) are seeded in 96-well plates. Following overnight incubation, cells are treated with varying concentrations of Avotaciclib hydrochloride (0-64 microM) for 48 hours. Cell viability is then assessed using a standard CCK-8 or MTT assay, and EC50 values (0.918, 0.580, 0.735, 0.662 microM) are calculated. Combination studies with PV-1019 are performed similarly.
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| Animal Protocol |
For Avotaciclib hydrochloride, in vivo efficacy studies are typically conducted in xenograft mouse models bearing human cancer cells (e.g., pancreatic or lung cancer). The compound is administered orally at optimized doses and schedules. Tumor volume is measured over time, and endpoints include tumor growth inhibition (TGI), body weight monitoring for tolerability, and ex vivo analysis of tumor tissue for CDK1 inhibition markers and apoptosis (e.g., cleaved caspase-3).
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| ADME/Pharmacokinetics |
Avotaciclib hydrochloride is characterized as an orally active CDK1 inhibitor, indicating good oral bioavailability in preclinical models. It can be used in research for pancreatic cancer and lung cancer, suggesting that its pharmacokinetic profile supports in vivo efficacy. Specific parameters such as Cmax, half-life, area under the curve (AUC), and oral bioavailability are typically determined in standard PK studies following oral or intravenous administration in rodent models.
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| Toxicity/Toxicokinetics |
Detailed toxicological profiles for Avotaciclib hydrochloride are not extensively documented in product literature. As a CDK1 inhibitor, potential on-target toxicities may include bone marrow suppression and gastrointestinal effects, consistent with other CDK inhibitors. Standard preclinical toxicology studies would be required to assess safety margins and tolerability prior to clinical development. The compound is currently in research phases for pancreatic cancer.
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| References | |
| Additional Infomation |
Avotaciclib hydrochloride (BEY1107 hydrochloride) is a hydrochloride salt form of Avotaciclib (CAS 1983983-41-0) with a molecular weight of 317.73. The free base has a molecular weight of 281.27. It is a potent and orally active CDK1 inhibitor that also shows effects on CDK4 and CDK6. The compound has been researched for locally advanced or metastatic pancreatic cancer and lung cancer, particularly radiotherapy-resistant non-small cell lung cancer when combined with checkpoint kinase inhibitors. No FDA or EMA approval has been granted to date.
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| Molecular Formula |
C13H12CLN7O
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| Molecular Weight |
317.73
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| Related CAS # |
Avotaciclib trihydrochloride;1983984-01-5;Avotaciclib;1983983-41-0
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| Appearance |
Light yellow to yellow solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.1473 mL | 15.7366 mL | 31.4733 mL | |
| 5 mM | 0.6295 mL | 3.1473 mL | 6.2947 mL | |
| 10 mM | 0.3147 mL | 1.5737 mL | 3.1473 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.
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