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PF-05212384

PF-05212384 Suppliers list
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Products Intro: Product Name:PKI-587
CAS:1197160-78-3
Purity:98%(Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
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Products Intro: Product Name:PF-05212384 (PKI-587)
CAS:1197160-78-3
Purity:98% Package:10MG;50MG;100MG,1G,5G,10G.100G
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Products Intro: Product Name:PF-05212384
CAS:1197160-78-3
Purity:99% Package:1kg;2USD
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Products Intro: Product Name:PF-05212384
CAS:1197160-78-3
Purity:98% HPLC LCMS Package:10G;20G
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Products Intro: Product Name:PF-05212384
CAS:1197160-78-3

PF-05212384 manufacturers

  • Gedatolisib
  • Gedatolisib pictures
  • $45.00 / 2mg
  • 2024-11-19
  • CAS:1197160-78-3
  • Min. Order:
  • Purity: 99.48%
  • Supply Ability: 10g
  • Gedatolisib;PKI-587
  • Gedatolisib;PKI-587 pictures
  • $200.00 / 1g
  • 2024-11-01
  • CAS:1197160-78-3
  • Min. Order: 1g
  • Purity: 98%+
  • Supply Ability: 100kgs
  • PF-05212384
  • PF-05212384 pictures
  • $2.00 / 1kg
  • 2019-07-06
  • CAS:1197160-78-3
  • Min. Order: 1kg
  • Purity: 99%
  • Supply Ability: 100kg
PF-05212384 Basic information
Description
Product Name:PF-05212384
Synonyms:PF-05212384;PKI587;N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea;1-(4-(4-(dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea;Gedatolisib (PF-05212384, PKI-587);N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea PF-05212384 (PKI-587);PKI-587 N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea;PKI-587 ( Gedatolisib )
CAS:1197160-78-3
MF:C32H41N9O4
MW:615.73
EINECS:
Product Categories:Akt;mTOR;PI3K;PI3K/Akt/mTOR;Inhibitors
Mol File:1197160-78-3.mol
PF-05212384 Structure
PF-05212384 Chemical Properties
Melting point 226-227°C
density 1.364
storage temp. Refrigerator
solubility DMSO
pka13.97±0.70(Predicted)
form Solid
color Off-White
Safety Information
HS Code 29349990
MSDS Information
PF-05212384 Usage And Synthesis
DescriptionGedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2.
Chemical PropertiesOff-White Solid
UsesThis compound shows inhibitory activity against PI3K-α, PI3K-γ and mTOR. Potent PI3K/mTOR Dual Inhibitor.
Biological Activitypf-05212384 is an inhibitor of pi3k/mtor with ic50 values of 0.4nm, 6nm, 8nm, 6nm and 1.4nm for pi3kα, pi3kβ, pi3kγ, pi3kδ and mtor, respectively [1].pf-05212384 is a pan-pi3k/mtorinhibitor and shows to be highly selective for pi3k and mtor. besides the wt p13k, pf-05212384 can also inhibit mutant p13k with ic50 values of 0.6nm for both h1047r and e545k mutants. in cellular assay, pf-05212384 potently inhibits tumor growth in mda-361 and pc3-mm2 cell lines with ic50 values of 4nm and 13.1nm, respectively. meanwhile, pf-05212384 suppresses the phosphorylation of pi3k/mtor signaling pathway proteins in cells. it inhibits the phosphorylation of akt as well as the akt effector proteins including gsk3 kinase, enos and pras 40. moreover, pf-05212384 has potent anti-tumor activity in a variety of xenograft models including h1975, bt474, hct116, h1975 and u87mg [1, 2]
Enzyme inhibitorThis dual PI3K/mTOR (phosphoinositide-3-kinase and mammalian target of rapamycin) signal-transduction pathway inhibitor and antineoplastic agent (F.Wt. = 615.73; CAS 1197160-78-3); Solubility (25°C): 2 mg/mL DMSO, <1 mg/mL Water), also known as PF-05212384 and systematically as 1-(4- (4-(dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino- 1,3,5-triazin-2-yl)phenyl)urea, inhibits PI3K-α, PI3K-γ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 also inhibits mutant forms of PI3Kα, including the PI3Kα-H1047R and PI3Kα-E545K with IC50 of 0.6 nM and 0.6 nM, respectively.
references[1] venkatesan a m, dehnhardt c m, delos santos e, et al. bis (morpholino-1, 3, 5-triazine) derivatives: potent adenosine 5′-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (pki-587), a highly efficacious dual inhibitor. journal of medicinal chemistry, 2010, 53(6): 2636-2645.
[2] mallon r, feldberg l r, lucas j, et al. antitumor efficacy of pki-587, a highly potent dual pi3k/mtor kinase inhibitor. clinical cancer research, 2011, 17(10): 3193-3203.
PF-05212384 Preparation Products And Raw materials
Tag:PF-05212384(1197160-78-3) Related Product Information
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