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CCT241533 hydrochloride

Cat. No. M5156

CCT241533 hydrochloride Structure

Synonym: CCT241533 HCl

Size Price Availability Quantity
5mg USD 160 In stock
10mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CCT241533 hydrochloride is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM. CCT241533 hydrochloride shows minimal cross-reactivity against a panel of kinases at 1 uM. CCT241533 HCl 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 HCl 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 478.94
Formula C23H27FN4O4.HCl
CAS Number 1431697-96-9
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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CCT241533 hydrochloride, CCT241533 HCl supplier, Checkpoint, inhibitors

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