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AdipoGen PF-0477736
SDP

Supplier:  AdipoGen AGCR13537M005

Encompass_Preferred

Chemical. CAS 952021-60-2. Formula C22H25N7O2. MW 419.5. PF-0477736 is a potent, selective ATP-competitive inhibitor of Chk1 Ki = 0.49nM with 100-fold selectivity over Chk2 Ki = 47nM. When used in combination with various chemotherapeutics e.g. gemcitabine and carboplatin, PF-0477736 abrogates DNA damage-induced cell cycle arrest, sensitizes cells to DNA damage, potentiating the antiproliferative effects of these compounds in vitro and in vivo in tumor cell lines and xenografts. PF-0477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3 and Ret Ki = 10, 14, 23, 23, 25 and 39 nM, respectively. Checkpoint kinase 1 Chk1 belongs to the Ca2/calmodulin-dependent protein kinase class of enzymes CAMK. CAMKs are activated by increases in the concentration of intracellular calcium ions Ca2 and calmodulin.

Catalog No. 50-256-2329


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