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Art. -Nr.: HY-190774

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INCB127443

INCB127443 is an orally active and selective CDK2/cyclin E1 inhibitor (IC₅₀ = 0.99 nM). INCB127443 is an ATP-competitive inhibitor that blocks Rb phosphorylation and cell cycle progression, and inhibits S-phase progression and proliferation in cyclin E-overexpressing ovarian cancer cells. INCB127443 shows antitumor efficacy and inhibits Rb phosphorylation in a cyclin E-overexpressing ovarian cancer xenograft model. INCB127443 can be used for research related to ovarian cancer.

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CAS. Nr.: 2602667-12-7
Formel: C₂₄H₂₆ClF₄N₇O₂S
Molecular Weight:588.02

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

INCB127443 Chemical Structure

CAS. Nr.: 2602667-12-7

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

CDK2/cyclin E1

0.99 nM (IC₅₀)

CDK1/cyclinB1

313 nM (IC₅₀)

Cdk4/cyclin D1

12 nM (IC₅₀)

CDK5/p35

243 nM (IC₅₀)

CDK6/D1

22 nM (IC₅₀)

cdk6/cyclin D3

85 nM (IC₅₀)

CDK7/H

143 nM (IC₅₀)

CDK9/T1

3511 nM (IC₅₀)

CDK12/K

748 nM (IC₅₀)

CDK13/K

7053 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
OVCAR-3	IC50	518 nM	Inhibition of CDK1-dependent NPM T199 phosphorylation in human OVCAR-3 cells. Inhibition of CDK1-dependent NPM T199 phosphorylation in human OVCAR-3 cells.	42911678
JeKo-1	IC50	445 nM	Inhibition of CDK4-dependent pRb in human JeKo-1 cells. Inhibition of CDK4-dependent pRb in human JeKo-1 cells.	42911678
CAL-51	IC50	448 nM	Inhibition of CDK4-dependent pRb in human CAL-51 cells. Inhibition of CDK4-dependent pRb in human CAL-51 cells.	42911678
MV4-11	IC50	416 nM	Inhibition of CDK6-dependent pRb in human MV-4-11 cells. Inhibition of CDK6-dependent pRb in human MV-4-11 cells.	42911678
OVCAR-3	IC50	27 nM	Inhibition of S-phase in human OVCAR-3 ovarian cancer cells treated with increasing concentrations of INCB127443. Inhibition of S-phase in human OVCAR-3 ovarian cancer cells treated with increasing concentrations of INCB127443.	42911678
OVCAR-3	IC50	46 nM	Inhibition of long-term proliferation in human OVCAR-3 cells measured by confluence-based IncuCyte assay over 14 days. Inhibition of long-term proliferation in human OVCAR-3 cells measured by confluence-based IncuCyte assay over 14 days.	42911678

In Vitro

Anti-cancerCell Cycle RegulationOthers

Anti-cancer

INCB127443 (14 days) exhibits a stronger inhibitory effect on the long-term proliferation of CCNE1-high COV318 and OVCAR-3 cells than on CCNE1-low COV504 cells^[1].

Anti-cancer

Cell Cycle Regulation

INCB127443 (1.5-10000 nM) potently induces S-phase inhibition in CCNE1-high COV318 and OVCAR-3 cells, whereas it shows lower potency in CCNE1-low COV504 cells^[1].

Cell Cycle Regulation

INCB127443 (compound 30) potently inhibits CDK2/cyclin E1 with an IC₅₀ of 0.99 nM and shows selectivity over CDK1 and other tested CDK/cyclin complexes; it potently binds CDK2/cyclin E1 in cells with an IC₅₀ of 5.9 nM^[1].
INCB127443 exhibits 20-25-fold cellular selectivity relative to CDK1, CDK4, and CDK6 in tested cells and whole blood models^[1].

Others

INCB127443 has a low intrinsic clearance in human microsomes, moderate Caco-2 permeability, an unbound plasma fraction of 8%, and high FaSSIF solubility^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	V_dss	AUC	C_max	F
Rat^[1]	3 mg/kg	p.o.	/	/	3518 nM·h	823 nM	94 %
Rat^[1]	0.5 mg/kg	i.v.	4.8 h	4.7 L/kg	/	/	/
Cynomolgus Monkey^[1]	1 mg/kg	p.o.	/	/	4695 nM·h	435 nM	64 %
Cynomolgus Monkey^[1]	0.3 mg/kg	i.v.	10 h	2.3 L/kg	/	/	/

In Vivo

Anti-cancer

INCB127443 (compound 30) (3-100 mg/kg; p.o.; twice daily; 5 days) dose-dependently inhibits tumor pRb S780 in CCNE1-high OVCAR-3 xenografts^[1].
INCB127443 (3-100 mg/kg; p.o.; twice daily or once daily; 24 days) produces dose-dependent antitumor activity in CCNE1-high OVCAR-3 xenograft tumors, with a tumor growth inhibition rate of 83% at 100 mg/kg twice daily^[1].

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

Animal Model:

athymic nude (female, 4-6-week, 1 × 10⁷ OVCAR-3 cells suspended in a 1:1 mixture of PBS and Matrigel)^[1]
Dosage:

3, 10, 30, 100 mg/kg
Administration:

p.o.; twice daily; 5 days
Result:

Produced dose-dependent inhibition of tumor pRb S780 in CCNE1-high OVCAR-3 xenografts, reaching 79% inhibition at 100 mg/kg twice daily.

Animal Model:

athymic nude (female, 4-6-week, 1 × 10⁷ OVCAR-3 cells suspended in a 1:1 mixture of PBS and Matrigel)^[1]
Dosage:

3, 10, 30, 100 mg/kg (twice daily)
100 mg/kg (once daily)
Administration:

p.o.; twice daily or once daily; 24 days
Result:

Reached 17% tumor growth inhibition at 3 mg/kg twice daily, 14% at 10 mg/kg twice daily, 65% at 30 mg/kg twice daily, 83% at 100 mg/kg twice daily, and 78% at 100 mg/kg once daily at study end.

Related Protocols :

Chemical Information

CAS. Nr. 2602667-12-7
Molecular Weight 588.02
Formel C₂₄H₂₆ClF₄N₇O₂S
SMILES

FC(C1=CN=C(NC2CCN(S(=O)(C)=O)CC2)N=C1C3=CN(C4=CC=C(CN5CCC5)C(F)=C4Cl)C=N3)(F)F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Mukai K, et al. Discovery of INCB127443: A Potent and Orally Available Inhibitor of Cyclin-Dependent Kinase 2. Journal of medicinal chemistry. 2026 Oct 22;69(20):23915-23946. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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INCB127443

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

IC50 & Target

Cellular Effect

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

INCB127443 Related Classifications

HY-190774 Related Classifications

Bioz

Keywords

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