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CCT241533

Cat. No. M5155
CCT241533 Structure
Size Price Availability
5mg USD 180 Out of stock
10mg USD 320 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CCT241533 is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM. CCT241533 shows minimal cross-reactivity against a panel of kinases at 1 uM. CCT241533 blocked CHK2 activity in human tumor cell lines in response to DNA damage, as shown by inhibition of CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation. CCT241533 did not potentiate the cytotoxicity of a selection of genotoxic agents in several cell lines. CCT241533 abolished the induction of the pS516 CHK2 signal, implying that the potentiation of PARP inhibitor cell killing by CCT241533 was due to inhibition of CHK2.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 442.48
Formula C23H27FN4O4
CAS Number 1262849-73-9
Purity >99%
Solubility DMSO 10 mM
Storage at -20°C
References

CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.
Anderson VE, et al. Cancer Res. 2011 Jan 15;71(2):463-72. PMID: 21239475.

Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
Caldwell JJ, et al. J Med Chem. 2011 Jan 27;54(2):580-90. PMID: 21186793.

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AZD7762 hydrochloride

AZD7762 hydrochloride is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CCT241533 supplier, Checkpoint, inhibitors

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