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CCT241533 hydrochloride

Cat. No. M5156
CCT241533 hydrochloride Structure
Synonym:

CCT241533 HCl

Size Price Availability
5mg USD 160  USD160 Out of stock
10mg USD 300  USD300 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 478.94
Formula C23H27FN4O4.HCl
CAS Number 1431697-96-9
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

[1] Anderson VE, et al. Cancer Res. CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.

[2] Caldwell JJ, et al. J Med Chem. Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.

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

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