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HY-10254

CAS:391210-10-9

 (Synonyms  PD325901)
391210-10-9  Technical Data: Price and Availability of  Cas No:391210-10-9

Cas : 391210-10-9 M.Wt: 482.1931
Cas : 391210-10-9 Formula: C16H14F3IN2O4
Cas : 391210-10-9 Purity: >98 %
Cas : 391210-10-9 Storage: at 20℃ 2 years
Cas : 391210-10-9 Solubility: DMSO: ≥ 56 mg/mL
Cas : 391210-10-9 Name: PD0325901
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10mg/$90 In-stock
25mg/$150 In-stock
50mg/$190 In-stock
100mg/$290 In-stock
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500mg/$940 In-stock
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391210-10-9  Data Sheet:
 
Introduction of 391210-10-9 :
PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. IC50 & Target: IC50: 0.33 nM (MEK) In Vitro: PF0325901 shows higher permeability, and should be able to achieve higher systemic exposures than CI-1040[1]. PD0325901 is exquisitely specific and highly potent against purified MEK, revealing a Kiapp of 1 nM against activated MEK1 and MEK2. PD0325901 is roughly 500-fold more potent than CI-1040 with respect to its cellular effects on phosphorylation of ERK1 and ERK2, displaying subnanomolar activity. PD0325901 prevents the growth of melanoma cell lines. PD0325901 inhibits the growth of TPC-1 cells and K2 cells with GC50 of 11 nM and 6.3 nM, respectively. PD0325901 significantly prevents the the growth of PTC cells harboring a BRAF mutation at very low concentration (10 nM) and only moderately increases the growth of the PTC cells carrying the RET/PTC1 rearrangement at the same concentration. PD0325901 effectively inhibits the phosphorylation of ERK1/2 in multiple PTC cell lines[2].? In Vivo: PD0325901 (25 mg/kg, p.o.) inhibits phosphorylation of ERK by more than 50% at 24 hours post-dosing. The dose required to produce a 70% incidence of complete tumor responses (C26 model) is 25 mg/kg/day versus 900 mg/kg/day for PD0325901 and CI-1040, respectively. Anticancer activity of PD 0325901 has been demonstrated for a broad spectrum of human tumor xenografts. PD0325901 (20-25 mg/kg/day, p.o.) treatment in mice, shows no tumor growth inoculated with PTC cells bearing a BRAF mutation.?For PTC with the RET/PTC1 rearrangement, the average tumor volume of the orthotopic tumor is decreased by 58% as compared with controls. PTC cells carrying a BRAF mutation are more sensitive to PD0325901 than are PTC cells carrying the RET/PTC1 rearrangement[2].
 
References on 391210-10-9 :
 

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