TC-A 2317 hydrochloride

Modify Date: 2024-01-07 11:50:55

TC-A 2317 hydrochloride Structure
TC-A 2317 hydrochloride structure
Common Name TC-A 2317 hydrochloride
CAS Number 1245907-03-2 Molecular Weight 392.92600
Density N/A Boiling Point N/A
Molecular Formula C19H29ClN6O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of TC-A 2317 hydrochloride


TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity[1].

 Names

Name 2-[(6-Hydroxy-6-methyl-2-heptanyl)amino]-4-methyl-6-[(5-methyl-1H -pyrazol-3-yl)amino]nicotinonitrile hydrochloride (1:1)
Synonym More Synonyms

 TC-A 2317 hydrochloride Biological Activity

Description TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity[1].
Related Catalog
Target

Aurora A:1.2 nM (Ki)

Aurora B:101 nM (Ki)

In Vitro TC-A 2317 hydrochloride (Compound 6) inhibits proliferation of HCT116 cells with an IC50 of 115 nM[1].
In Vivo TC-A 2317 hydrochloride is effective in antitumor mice model without decrease of body weight[1]. TC-A 2317 hydrochloride shows good PK profile; Cmax value is 4930 nM (Tmax=1.2 h) and serum concentration after 24 h is 52 nM (T1/2=3.3 h) at 30 mg/kg po in rats[1]. Animal Model: HCT-116 Xenograft mice mode[1] Dosage: P.o.; daily for 14 days Administration: 30 mg/kg Result: Growth of tumor was inhibited by 59% after 14 days.
References

[1]. Ando R, et al. 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors. Bioorg Med Chem Lett. 2010;20(15):4709-4711.

 Chemical & Physical Properties

Molecular Formula C19H29ClN6O
Molecular Weight 392.92600
Exact Mass 392.20900
PSA 112.88000
LogP 4.07528

 Synonyms

TC-A 2317 hydrochloride