Order Information
Contact us
Insert title here
Featured Products
HY-100001  |  SKF-96365 (hydrochloride)
HY-100002  |  ML162
HY-100003  |  ML210
HY-100004  |  Fumarate hydratase-IN-1
HY-100005  |  Fumarate hydratase-IN-2
HY-100006  |  MRT68921
HY-100007  |  TAK-438 (free base)
HY-100008  |  Peretinoin
HY-100009  |  Ufenamate
HY-10001  |  Calcipotriol
HY-100010  |  Sulfathiourea
HY-100011  |  SR-3029
HY-100012  |  CBR-5884
HY-100013A  |  (1R,2R)-2-PCCA
HY-100013B  |  (1S,2S)-2-PCCA
HY-100014  |  KDM5A-IN-1
HY-100015  |  Mivebresib
HY-100016  |  AZD0156
HY-100017  |  BAY-876
HY-100018  |  BAY1125976


952021-60-2  Technical Data: Price and Availability of  Cas No:952021-60-2

Cas : 952021-60-2 M.Wt: 419.4796
Cas : 952021-60-2 Formula: C22H25N7O2
Cas : 952021-60-2 Purity: >98 %
Cas : 952021-60-2 Storage: at 20℃ 2 years
Cas : 952021-60-2 Solubility: 10 mM in DMSO
Cas : 952021-60-2 Name: PF 477736
Please check here to inquiry for availability and price .

952021-60-2  Data Sheet:
Introduction of 952021-60-2 :
PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes; shows ~100-fold selectivity for Chk1 than Chk2. IC50 value: 0.49 nM (Ki) [1] Target: Chk1 in vitro: PF-477736 (128 nM) abrogates the camptothecin-induced DNA damage checkpoint in a dose-dependent manner in CA46 and HeLa cells. PF-477736 effectively abrogates the gemcitabine-induced S-phase arrest with a corresponding increase in apoptotic cell populations in HT29 cells. PF-477736 (540 nM) enhances gemcitabine-induced cytotoxicity in a time- and dose-dependent manner in HT29 cells. PF-477736 potentiates the growth-inhibitory activity of a panel of chemotherapeutic agents across a broad spectrum of p53-deficient human cancer cell lines in the MTT assay. Addition of PF-477736 (360 nM) to gemcitabine-arrested cells induces a dramatic increase in the intensity of H2AX phosphorylation, reflecting a greater number of γ-H2AX molecules near sites of DNA damage [1]. PF-477736 (0.5 nM) selectively blocks p73 and P53 phosphorylation in presence of curcumin in HL-60 cells [2]. PF-477736 (360 nM) suppresses docetaxel-induced phosphorylation of histone H3 (Ser10) and Cdc25C (Ser216) and potentiates apoptosis in COLO205 cells. [3] PF-477736 (250 nM) combined with MK-1775 has marked synergistic cytotoxic activity in OVCAR-5 cells. PF-477736 (250 nM) combined with MK-1775 causes accumulation of cells with a DNA content between 2N and 4N in OVCAR-5 cells. PF-477736 (250 nM) combined with MK-1775 causes premature mitosis before the end of DNA replication, with damaged DNA leading to apoptotic cell death in OVCAR-5 cells [4]. in vivo: PF-477736 (4 mg/kg i.v.) results in terminal half-life (T1/2) of 2.9 hours, AUC of 5.72 μg×hr/mL and CLp of 11.8 mL/min/kg in rats. PF-477736 dose-dependently enhances the antitumor activity of a maximum tolerated dose of gemcitabine in the Colo205 xenograft mouse model. PF-477736 (12 mg/kg) induces an increase in the phosphorylation of histone H3 (Ser10) and of phospho-histone H2AX in the Colo205 xenograft mouse model [1]. PF-477736 (15 mg/kg i.p.) enhances docetaxel induced tumor growth inhibition and tumor growth delay in COLO205 and MDA-MB-231 xenograft models [3]. PF 477736 (10 mg/kg once daily i.p.) combined with MK-1775 (30 mg/kg twice a day oral) leads to greater tumor growth inhibition in mice bearing OVCAR-5 xenografts [4].
References on 952021-60-2 :

Keywords: buy PF 477736 | PF 477736 Supplier | purchase PF 477736 | PF 477736 cost | PF 477736 manufacturer | order PF 477736 | PF 477736 distributor | PF 477736 structure
buy 952021-60-2 | 952021-60-2 Supplier | purchase 952021-60-2 | 952021-60-2 cost | 952021-60-2 manufacturer | order 952021-60-2 | 952021-60-2 distributor | 952021-60-2 structure
Insert title here
Products are for research use only. Not for human use. We do not sell to patients.           Copyright © 2009 Haoyuan Chemexpress All Rights Reserved
ADDRESS: 6/F, No. 2 Building, No. 720,Cailun Road, Shanghai, P.R.China  
86-21-58998590   FAX: 86-21-53700326, 86-21-58998590   E-mail: sales@chemexpress.cn