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PF 477736

Catalog #: 4277
3 Citations Datasheet
Catalog # Availability Size / Price Qty
4277/10
4277/50
PF 477736 | CAS No. 952021-60-2 | Checkpoint Kinase Inhibitors
1 Image
Description: Selective Chk1 inhibitor
Alternative Names: PF-0044736

Chemical Name: (R)-α-Amino-N-[5,6-dihydro-2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-1H-pyrrolo[4,3,2-ef][2,3]benzodiazepin-8-yl]-cyclohexaneacetamide

Purity: ≥99%

Product Details
Citations (3)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

PF 477736 is a selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively). Abrogates cell cycle arrest at S and G2-M checkpoints; sensitizes cells to DNA damage. Enhances docetaxel (Cat. No. 4056) efficacy in tumor cells and xenografts.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 477736 is reviewed on the chemical probes website.

Technical Data

M.Wt:
419.48
Formula:
C22H25N7O2
Solubility:
Soluble to 75 mM in DMSO
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
952021-60-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

Background References

  1. Inhibiting checkpoint kinase 1 protects bone from bone resorption by mammary tumor in a mouse model
    S Liu, Y Liu, K Minami, A Chen, Q Wan, Y Yin, L Gan, A Xu, N Matsuura, M Koizumi, Y Liu, S Na, J Li, H Nakshatri, BY Li, H Yokota
    Oncotarget, 2018;9(10):9364-9378.
  2. DNA damage detection and repair pathways - recent advances with inhibitors of checkpoint kinases in cancer therapy.
    Ashwell and Zabludoff
    Clin.Cancer Res., 2008;14:4032
  3. Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1.
    Blasina et al.
    Mol.Cancer Ther., 2008;7:2394
  4. PF-00477736 mediates checkpoint kinase 1 signaling pathways and potentiates docetaxel-induced efficacy in xenografts.
    Zhang et al.
    Clin.Cancer Res., 2009;15:4630

Product Datasheets

Citations for PF 477736

The citations listed below are publications that use Tocris products. Selected citations for PF 477736 include:

3 Citations: Showing 1 - 3

  1. Replication stress promotes cell elimination by extrusion.
    Authors: Daniel P Et al.
    Nature  2021;593:591-596
  2. Histone variant H3.3 residue S31 is essential for Xenopus gastrulation regardless of the deposition pathway.
    Authors: Damarys Et al.
    Nat Commun  2020;11:1256
  3. Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition.
    Authors: Meng Et al.
    J Exp Med  2015;15:422

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