2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK4/6-IN-14

CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases.

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CDK4/6-IN-14 Chemical Structure

CDK4/6-IN-14 Chemical Structure

CAS No. : 2699091-15-9

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CDK4/6-IN-14 Related Antibodies

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Description

CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases[1].

IC50 & Target[1]

CDK4

10 nM (IC50)

CDK6

16 nM (IC50)

CDK1

>10000 nM (IC50)

CDK2

1045 nM (IC50)

CDK7

2595 nM (IC50)

CDK9

2664 nM (IC50)

In Vitro

CDK4/6-IN-14 (compound 42; 1-6 μM; 5 days) exhibits potent inhibitory activity against the proliferation of breast cancer MCF-7, T47D, and ZR-75-1 cell lines. CDK4/6-IN-14 significantly inhibits growth and clone formation of MCF-7 and T47D cells[1].
CDK4/6-IN-14 (compound 42; 1-6 μM) arrests the cell cycle at the G1 phase of MCF-7 and T47D cells in the dose-dependent manner[1].
CDK4/6-IN-14 (compound 42; 1-6 μM; 24 hours) significantly inhibits the phosphorylation of retinoblastoma (RB), while the expression of RB protein was almost unchanged. In addition, CDK4/6-IN-14 exhibits a concentration-dependent effect to decrease the level of c-MYC and cyclin D1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CDK4/6-IN-14 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 and T47D cells
Concentration: 1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells)
Incubation Time: 5 days
Result: Significantly inhibited growth and clone formation of MCF-7 and T47D cells.

Western Blot Analysis[1]

Cell Line: MCF-7 and T47D cells
Concentration: 1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells)
Incubation Time: 24 hours
Result: Significantly inhibited the phosphorylation of RB.
In Vivo

CDK4/6-IN-14 (compound 42; 100-150 mg/kg; p.o; once a day; for 23 days) significantly inhibits tumor growth of the MCF-7 xenograft model[1].
CDK4/6-IN-14 (compound 42) exhibits a suitable t1/2 of intravenous and oral administration (2.62 and 3.59 h, respectively). Moreover, the oral bioavailability of CDK4/6-IN-14 is 43%[1].
Pharmacokinetic Parameters of CDK4/6-IN-14 (Compound 42) in Sprague–Dawley Rats[1].

admin. Cmax (ng/mL) AUC0-∞ (h × ng/mL) MRT0-∞ (h) Tmax (h) t1/2 (h) F (%)
IV 290.52 372.56 3.50 0.033 2.62
PO 144.11 1612.18 9.11 6 3.59 43
Dose: i.v. at 1 mg/kg; p.o. at 10 mg/kg[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice bearing MCF-7 cells[1]
Dosage: 100 mg/kg, 150 mg/kg
Administration: Orally administertion; once a day; for 23 days
Result: Significantly inhibited tumor growth of the MCF-7 xenograft model.
Molecular Weight

483.97

Formula

C24H27ClFN7O
CAS No.
SMILES

O=C1N(CC)CCC2=C1C=CC(C3=NC(NC4=NC=C(N5CCNCC5)C=C4)=NC=C3F)=C2.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CDK4/6-IN-14 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK4/6-IN-142699091-15-9CDKCyclin dependent kinaseCDK4CDK6anticancer effectretinoblastomac-MYCcyclin D1Inhibitorinhibitorinhibit

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