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Art. -Nr.: HY-128766

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CHK1-IN-4

CHK1-IN-4 is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC₅₀ ≤ 1 nM. The IC₅₀ value of CHK1-IN-4 against Chk2 ranges from 50 to 100 nM. CHK1-IN-4 inhibits cancer cell proliferation and exhibits antitumor activity in colon cancer xenograft models. CHK1-IN-4 can be used for the research of colon cancer and breast cancer.

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CAS. Nr.: 2120398-41-4
Formel: C₁₈H₁₈BrN₇O₂
Molecular Weight:444.29

Speicherung:

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

Data Sheet (271 KB)

CHK1-IN-4 Chemical Structure

CAS. Nr.: 2120398-41-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Chk1

≤ 1 nM (IC₅₀)

Alle Checkpoint Kinase (Chk) Isoform-spezifische Produkte anzeigen :

In Vitro

CHK1-IN-4 (Compound 3) inhibits the proliferation of HT-29 colon cancer cells and MDA-MB-231 breast cancer cells, with IC₅₀ values ranging from 10-50 nM and 50-100 nM, respectively^[1].
CHK1-IN-4 (0.4-33.3 nM; 16.5-27 h) potently inhibits SN-38 (HY-13704)-induced Chk1^S296 phosphorylation in HT-29 colon cancer cells^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_0-t	AUC_0-inf	MRT	V_d	V_ss	CL
Rat^[1]	10 mg/kg	i.v.	3.8 h	4531 ng/mL·h	4637 ng/mL·h	2.8 h	12.3 L/kg	6.4 L/kg	2.3 L/h/kg

In Vivo

CHK1-IN-4 (Compound 3) (40 mg/kg; intravenous injection; twice weekly) exhibits potent tumor growth inhibitory activity in the HT-29 colon cancer xenograft model^[1].
CHK1-IN-4 (10-40 mg/kg; intravenous injection; twice weekly) exhibits dose-dependent tumor growth inhibition in the LoVo colon cancer xenograft model^[1].

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

Chemical Information

CAS. Nr. 2120398-41-4
Molecular Weight 444.29
Formel C₁₈H₁₈BrN₇O₂
SMILES

N#CC1=NC=C(NC2=NNC(C3=C(OC)C=C(Br)C=C3OCCCN)=C2)N=C1
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

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.

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.

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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CHK1-IN-4

Alle Checkpoint Kinase (Chk) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CHK1-IN-4 Related Classifications

HY-128766 Related Classifications