| 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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| Other Sizes |
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| Targets |
CDK4 3 nM (IC50) CDK6 0.279 μM (IC50) CDK2 3.335 μM (IC50)
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|---|---|
| ln Vitro |
Furthermore, CDK4/6-IN-15 (compound 91) (10 μM; 24 h) potently suppresses MYLK4 and FLT3 with >90% inhibition rates.[1]. With GI50s of 0.107 μM (MV4-11) and 0.325 μM (MDA-MB-453), CDK4/6-IN-15 (0-5 μM; 72 h) selectively inhibits the growth of tumor cells[1]. In Rb-positive MV4-11 and MDA-MB-453 cells, CDK4/6-IN-15 (0.1–1 μM; 24 h) solely stops the cell cycle at the G1 phase[1]. MV4-11 and MDA-MB-453 cells undergo apoptosis in response to CDK4/6-IN-15 (0.1-1 μM or 0.3-3 μM; 24-96 h)[1]. Rb phosphorylation is inhibited by CDK4/6-IN-15 (0.1-3.3 μM; 4-24 h)[1].
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| ln Vivo |
CDK4/6-IN-15 (compound 91) exhibits oral comparable absorption in adult male BALB/c mice (20–25 g) in good health, as well as in male albino Wistar rats (250–350 g) (5 mg/kg for iv or 200 mg/kg for po; single dose)[1]. Path Dose (mg/kg) CL (mL/min /kg) Vss (L/kg) AUC (μM·h) Cmax (μM) Tmax (h) t1/2 (h) F (%) rat IV 5 155 27.5 1.2 1.4 / 2.1 / PO 20 / / 4.4 0.3 4.3 20.3 95 mouse IV 2 90 15.7 0.7 1.3 / 2.9 / PO 10 / / 4.3 0.6 2.5 2.7 129 [pharmacokinetic Analysis]
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: MV4-11 and MDA-MB-453 cells Tested Concentrations: 0.1 μM, 0.5 μM, and 1 μM for MV4-11; 0.3 μM, 0.6 μM, and 3.3 μM for MDA-MB-453 cells Incubation Duration: 24 h, 48 h, 72 h, and 96 h Experimental Results: Induced cell apoptosis via arresting cell cycle at G1 accompanied with Rb) phosphorylation suppression and E2F- regulated gene expression decreases. Western Blot Analysis[1] Cell Types: MV4-11 (GI50=0.107 μM) and MDA-MB-453 (GI50=0.325 μM) Tested Concentrations: 1×, 5×, 10× GI50 Incubation Duration: 4 h, 12 h, and 24 h Experimental Results: Resulted inhibition of Rb phosphorylation at S780. |
| 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.
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| Molecular Formula |
C21H27FN8S
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|---|---|
| Molecular Weight |
442.56
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| CAS # |
2078047-99-9
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
S1C(NC)=NC(C)=C1C1=C(C=NC(=N1)NC1=CC=C(C=N1)N1CCC(CC1)N(C)C)F
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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 : 5 mg/mL (11.30 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.13 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 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2596 mL | 11.2979 mL | 22.5958 mL | |
| 5 mM | 0.4519 mL | 2.2596 mL | 4.5192 mL | |
| 10 mM | 0.2260 mL | 1.1298 mL | 2.2596 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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