Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.

Product information

CAS Number: 2120398-39-0

Molecular Weight: 387.41

Formula: C18H22FN7O2

Chemical Name: 5-({5-[2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl]pyrazolidin-3-yl}amino)pyrazine-2-carbonitrile

Smiles: COC1=CC(F)=CC(OCCCN)=C1C1CC(NN1)NC1=CN=C(C=N1)C#N

InChiKey: OECWXHGRBWTUAM-UHFFFAOYSA-N

InChi: InChI=1S/C18H22FN7O2/c1-27-14-5-11(19)6-15(28-4-2-3-20)18(14)13-7-16(26-25-13)24-17-10-22-12(8-21)9-23-17/h5-6,9-10,13,16,25-26H,2-4,7,20H2,1H3,(H,23,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Chk1-IN-5 (compound 3; 0.4, 1.2, 3.7, 11.1, 33.3, 100 nM) inhibits Chk1 phosphorylation in the HT-29 colon cells.

In Vivo:

Chk1-IN-5 (compound 3; 40 mg/kg; IV; twice a week for 21 days) inhibits tumor growth in Baib/c nude mice with HT-29 colon cancer cells. Chk1-IN-5 (10 mg/kg; via tail vein intravenous injection) displays a longer half-life (T1/2=3.8 hours) and higher exposure (CL=2.3 L/hr•kg; Vss=6.4 L/kg; AUC=4531 ng/ml•h).

Products are for research use only. Not for human use.