CDK4/6-IN-15 hydrochloride |
| Catalog No.GC73086 |
CDK4/6-IN-15 hydrochloride es un inhibidor de CDK4/6 activo y selectivo por vía oral.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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CDK4/6-IN-15 drochloride is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 drochloride potently inhibits cancer cells growth. CDK4/6-IN-15 drochloride arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression.
CDK4/6-IN-15 (compound 91) (10 μM; 24 h) also potently inhibits FLT3 and MYLK4 with inhibition rates >90%[1].CDK4/6-IN-15 (0-5 μM; 72 h) suppresses tumour cell proliferation selectively with GI50s of 0.107 μM (MV4-11) and 0.325 μM (MDA-MB-453)[1].CDK4/6-IN-15 (0.1-1 μM; 24 h) arrests exclusively the cell cycle at G1 phase in Rb-positive MV4-11 cells and MDA-MB-453 cells[1].CDK4/6-IN-15 (0.1-1 μM or 0.3-3 μM; 24-96 h) triggers apoptosis in MV4-11 and MDA-MB-453 cells[1].CDK4/6-IN-15 (0.1-3.3 μM; 4-24 h) inhibits phosphorylation of Rb[1].
CDK4/6-IN-15 (compound 91) (2 mg/kg for i.v. or 10 mg/kg for p.o.; single dose) shows comparable oral absorption in healt male adult BALB/c mice (20-25 g) as well as (5 mg/kg for i.v. or 200 mg/kg for p.o.; single dose) in male albino Wistar rats (250-350 g)[1].Pharmacokinetic Analysis[1]
References:
[1]. Tadesse S, et al. Discovery and pharmacological characterization of a novel series of highly selective inhibitors of cyclin-dependent kinases 4 and 6 as anticancer agents. Br J Pharmacol. 2018 Jun;175(12):2399-2413.
| Cas No. | SDF | ||
| Formula | C21H28ClFN8S | M.Wt | 479.02 |
| Solubility | Storage | 4°C, protect from light, stored under nitrogen | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0876 mL | 10.438 mL | 20.876 mL |
| 5 mM | 0.4175 mL | 2.0876 mL | 4.1752 mL |
| 10 mM | 0.2088 mL | 1.0438 mL | 2.0876 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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