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CCT244747

Catalog No. T14904 CAS 1404095-34-6

CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 nM).

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CCT244747, CAS 1404095-34-6

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2 mg	5 days	$ 76.00

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Chemical Properties

Storage & Solubility Information

Description	CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 nM).
Targets&IC50	Chk1:7.7 nM
In vitro	CCT244747 demonstrates selective inhibition potential, performing poorly against CHK2 and CDK1 with IC50 values above 10 μM, whereas it more effectively inhibits FLT3 with an IC50 of 600 nM. It also significantly inhibits CHK1 cellular function, showing IC50s between 29 nM and 170 nM across various cell lines including HT29, SW620, MiaPaCa-2, and Calu6, with GI50s ranging from 0.33 μM to 3 μM. At a concentration of 0.3 μM, CCT244747 blocks CHK1 activity induced by SN38 and gemcitabine in HT29 and SW620 colon cancer lines, which leads to bypassing cell cycle arrest, alongside DNA damage and apoptosis induction. It exhibits robust inhibition (>80%) against a range of enzymes such as CHK1, RSK1, RSK2, AMPK, BRSK1, IRAK1, and TrkA. Additionally, CCT244747 enhances the sensitivity of bladder and head and neck cancer cells to radiation at concentrations between 0.5 and 2.0 μM and overcomes genotoxic-induced S and G2 arrest in colon cancer cell lines at 0.5 μM. At higher concentrations (10 μM), it shows less than 25% inhibition towards a spectrum of ion channels, including hNav1.5, hKv4.3/hKChIP2, hCav1.2, hKv1.5, hKCNQ1/hminK, and hHCN4.
In vivo	CCT244747, administered orally at doses ranging from 100 to 300 mg/kg, effectively inhibits the gemcitabine-induced phosphorylation of CHK1 at S296 for up to 24 hours in HT29 colon tumor xenografts. At a dosage of 75 mg/kg, CCT244747 enhances the antitumor effects of gemcitabine in both HT29 colon tumor and Calu6 human lung cancer xenografts. A regimen of CCT244747 at 100 mg/kg once daily for 7 days significantly reduces tumor burden in various human tumor xenografts. Additionally, at a dose of 100 mg/kg, CCT244747 demonstrates radiosensitization activity in Cal27 xenografts. When administered at 150 mg/kg, CCT244747 also exhibits potent antitumor activity in combination with irinotecan in SW620 human colon tumor xenografts.

Molecular Weight	408.46
Formula	C20H24N8O2
CAS No.	1404095-34-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (244.82 mM), Sonication is recommended.

References and Literature

1. Lainchbury M, et al. Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. J Med Chem. 2012 Nov 26;55(22):10229-40. 2. Walton MI, et al. CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs. Clin Cancer Res. 2012 Oct 15;18(20):5650-61. 3. Patel R, et al. An orally bioavailable Chk1 inhibitor, CCT244747, sensitizes bladder and head and neck cancer cell lines to radiation. Radiother Oncol. 2017 Mar;122(3):470-475.

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Keywords

CCT244747 1404095-34-6 Cell Cycle/Checkpoint Chk CCT-244747 CCT 244747 inhibitor inhibit

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