[CAS NO. 2078047-99-9] CDK4/6-IN-15
PRODUCTS SPECIFICATIONS [2078047-99-9]
DESCRIPTION [2078047-99-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 442.56 |
| Molecular Formula | C21H27FN8S |
| SMILES | CNC1=NC(C)=C(C2=NC(NC3=NC=C(N4CCC(N(C)C)CC4)C=C3)=NC=C2F)S1 |
Summary
IC50 & Target
|
CDK4 3 nM (IC 50 ) |
CDK6 0.279 μM (IC 50 ) |
CDK2 3.335 μM (IC 50 ) |
In Vitro
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 GI
50
s 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [1]
| Cell Line: | MV4-11 and MDA-MB-453 cells |
| Concentration: | 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 Time: | 24 h, 48 h, 72 h, and 96 h |
| Result: | 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 Line: | MV4-11 (GI 50 =0.107 μM) and MDA-MB-453 (GI 50 =0.325 μM) |
| Concentration: | 1×, 5×, 10× GI 50 |
| Incubation Time: | 4 h, 12 h, and 24 h |
| Result: | Resulted inhibition of Rb phosphorylation at S780. |
In Vivo
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 healthy 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]
| Route | Dose (mg/kg) | CL (mL/min/kg) | V ss (L/kg) | AUC (μM·h) | C max (μM) | T max (h) | t 1/2 (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 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.