| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
CDK4 CDK6
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|---|---|
| ln Vitro |
In the plasma of healthy persons, the metabolite M18 hydrochloride of abelacilb has a T1/2 of 43.1 hours [3]. The primary mode of action of CDK4/6 inhibitors is to cause cell cycle arrest by blocking the phosphorylation of the retinoblastoma (RB) protein. Other modifications to cancer cell biology are made by CDK4/6 inhibitors [4].
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| ln Vivo |
CDK4/6 inhibitors enhanced T cell survival and immunological memory in mice given tumor-specific CD8+ T cells [5].
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| References |
[1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non–Small Cell Lung Cancer: A Phase Ib Study.
[2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1. [3]. Palaniappan, et al. Abstract CT153: Pharmacokinetic drug interactions between abemaciclib and CYP3A inducers and inhibitors. Cancer Res. 2016-7-15; 76 (14_Supplement): CT153. [4]. Goel S, et al. CDK4/6 Inhibition in Cancer: Beyond Cell Cycle Arrest. Trends Cell Biol. 2018 Nov;28(11):911-925. |
| Molecular Formula |
C25H29CLF2N8O
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|---|---|
| Molecular Weight |
531.00
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| CAS # |
2704316-82-3
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| Related CAS # |
Abemaciclib metabolite M18-d8;Abemaciclib metabolite M18;2704316-81-2
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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 : 125 mg/mL (235.40 mM)
H2O : 100 mg/mL (188.32 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (94.16 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8832 mL | 9.4162 mL | 18.8324 mL | |
| 5 mM | 0.3766 mL | 1.8832 mL | 3.7665 mL | |
| 10 mM | 0.1883 mL | 0.9416 mL | 1.8832 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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