PF-05212384
Description- Product Name
- PF-05212384
- CAS No.
- 1197160-78-3
- Chemical Name
- PF-05212384
- Synonyms
- CS-46;PKI587;PF-05212384;PKI 587 PF 05212384;GEDATOLISIB;PKI-587;PF-05212384 (PKI-587);PF-05212384 USP/EP/BP;GEDATOLISIB;PF-05212384;PKI-587 ( Gedatolisib );Gedatolisib (PF-05212384, PKI-587)
- CBNumber
- CB32500950
- Molecular Formula
- C32H41N9O4
- Formula Weight
- 615.73
- MOL File
- 1197160-78-3.mol
PF-05212384 Property
- Melting point:
- 226-227°C
- Density
- 1.364
- storage temp.
- Refrigerator
- solubility
- DMSO
- pka
- 13.97±0.70(Predicted)
- form
- Solid
- color
- Off-White
Safety
- HS Code
- 29349990
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 14567
- Product name
- PF-05212384
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 14567
- Product name
- PF-05212384
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- 14567
- Product name
- PF-05212384
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $283
- Updated
- 2024/03/01
- Product number
- 4823
- Product name
- PF05212384
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $275
- Updated
- 2021/12/16
- Product number
- D461135
- Product name
- N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N''-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]-urea
- Packaging
- 50mg
- Price
- $670
- Updated
- 2021/12/16
PF-05212384 Chemical Properties,Usage,Production
Description
Gedatolisib (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 Properties
Off-White Solid
Uses
This compound shows inhibitory activity against PI3K-α, PI3K-γ and mTOR. Potent PI3K/mTOR Dual Inhibitor.
Biological Activity
pf-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 inhibitor
This 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
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View Lastest Price from PF-05212384 manufacturers
- Product
- Gedatolisib;PKI-587 1197160-78-3
- Price
- US $200.00-0.00/g
- Min. Order
- 1g
- Purity
- 98%+
- Supply Ability
- 100kgs
- Release date
- 2021-05-24
- Product
- PF-05212384 1197160-78-3
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-24