BiochemProbe — Life Science Research Reagents

Chk1-IN-6 free base · Synonyms: CPDP801758

Chk1-IN-6 is a selective and orally active Chk1 inhibitor.

For research use only. Not for human or veterinary use.

Target Checkpoint Kinase (Chk)
Research area Cancer
Purity >98% Stock Inquire
Data Sheet SDS COA

Chk1-IN-6 structure

CAS No.: 2428423-77-0

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
10 mg USD 480.00 BP-02014-10mg In stock Get quote
25 mg USD 960.00 BP-02014-25mg In stock Get quote
50 mg USD 1,520.00 BP-02014-50mg In stock Get quote
100 mg USD 2,320.00 BP-02014-100mg In stock Get quote
500 mg Inquire BP-02014-500mg Inquire Inquire

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Description

Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC50 of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine. Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma.

Biological activity

In Vitro Chk1-IN-6 (Compound 6c) shows antiproliferative activity of MV-4-11 and Z138 cells with IC50 values of 0.14 and 3.28 μM[1]. Chk1-IN-6 (0-5 nM, 72 h) combined with Gemcitabine shows a synergistic effect on HT-29, A549, and RPMI-8226[1]. Chk1-IN-6 (0-800 nM, 2 h) inhibits the phosphorylated S296 CHK1 (pS296 CHK1) and induces the phosphorylated S345 CHK1 (pS345 CHK1) in MV-4-11[1]. In Vivo k1-IN-6 (Compound 6c) (5-30 mg/kg, p.o., once daily for 21 days) significantly inhibits tumor growth in vivo in a dose-dependent manner in the MV-4-11 xenograft mouse model[1]. Chk1-IN-6 (5-30 mg/kg, p.o., continuously for 5 days/week for 22 days) shows synergistic anticancer effect of with Gemcitabine in the HT-29 xenograft mouse model[1].

Identifiers

SMILES
N#CC(C=C1)=NC=C1NC2=NC=C(C(F)(F)F)C(NCCC(C)(C)N)=N2
InChIKey
QCHCXIAOYLDHOY-UHFFFAOYSA-N

Specifications

MW (average)
365.3562
Formula
C16H18F3N7
CAS No.
2428423-77-0
Physical state
Solid
Color
White to off-white
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month.

Solubility

Soluble in DMSO : 25 mg/mL

Documents

References

[1]. Jin T, et al. Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile. J Med Chem. 2021 Oct 28;64(20):15069-15090.

Same target

Search Checkpoint Kinase (Chk)

Same research area

Search Cancer