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작성일 : 14-01-20
[Chemdea] PI3K/mTOR Inhibitors (2)
Compound 15e Dihydrochloride – PI3Ka Inhibitor / GDC-0941 – PI3Ka/d Inhibitor / 17-b-Hydroxywortmannin (HWT) / IC87114 - PI3Kδ Inhibitor / LY 294002 – PI3K Inhibitor
PI3K/mTOR Inhibitors (2)
 
 
Product Name: Compound 15e Dihydrochloride – PI3Ka Inhibitor
 
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A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-Ks
(p110a IC50 = 2 nM, p110b IC50 = 16 nM, p110g IC50 = 660 nM, and PI 3-K C2b IC50 = 220 nM) and inhibits non-PI 3-K
kinases only at much higher concentrations (IC50 ≥3.4 µM for Cdk2/E, KDR, PKA, and PKCa). Shown to inhibit cell
proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50 <3 µM) in A375 melanoma cells.
 
Details
Chemical Formula:
 
C16H15N3O2S*2HCl
CAS No.:
 
371943-05-4
Molecular weight:
 
386.3
Purity:
≥99% by HPLC
Appearance:
 
White solid
Chemical name:
 
3-(4-Morpholinothieno[3,2-d]pyrimidin-2-yl)phenol dihydrochloride
Solubility:
 
DMSO (10mg/mL). The free base form of this compound (Cat# CD0189) is 2.5-fold
more soluble.
Storage:
Protect from light. Packaged under inert gas
 
Reference
 
 
Product Name: GDC-0941 – PI3Ka/d Inhibitor
 
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Potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) under clinical trials, with p110α IC50 = 3 nM, 
p110b IC50 =33 nM, p110d IC50 =3 nM, p110g IC50 =75 nM, DNA-PK IC50 =1230 nM and mTOR IC50 =580 nM.
 
Details
Chemical Formula:
 
C23H27N7O3S2
CAS No.:
 
957054-30-7
Molecular weight:
 
513.6
Purity:
99% by HPLC
Appearance:
 
White solid
Chemical name:
 
2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-thieno[3,2- d]pyrimidine
Solubility:
 
DMSO (66mg/mL). Note: the bismesylate form marketed by other vendors is poorly soluble
in organic solvents and water.
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Product Name: 17-b-Hydroxywortmannin (HWT)
 
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A cell-permeable Wortmannin 17β-Hydroxy analog (HWT) that acts as an irreversible PI 3-K inhibitor with an 8.4-fold
higher potency than that of Wortmannin (IC50 = 0.5 and 4.2 nM, respectively) and inhibits mTOR only at much higher 
concentrations (IC50 = 0.193 µM). Both Wortmannin and HWT covalently modify a conserved lysine residue (Lys833 in
porcine PI 3-Kγ) in the PI 3-K ATP binding pocket via their electrophilic furan ring at C-20 position. HWT is shown to
effectively arrest the growth of LNCaP cells (IC50 = 1.464 µM) in vitro, however, its high in vivo toxicity renders it 
unsuitable for tumor killing studies in mice. Also reported to inhibit late phase PLD-mediated PA production upon fMLP
stimulation of human neutrophils. See also our product PX-866-17OH (Cat # CD0323) and PX-13-17OH (Cat # CD0305
with similar activity.
 
Details
Chemical Formula:
 
C23H26O8
CAS No.:
 
58053-83-1
Molecular weight:
 
430.5
Purity:
99% by HPLC
Appearance:
 
Off White solid
Chemical name:
 
17-b-Hydroxywortmannin (LY 301497)
Solubility:
 
DMSO (100mg/mL)
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Product Name: IC87114 - PI3Kδ Inhibitor
 
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A cell permeable, selective inhibitor of PI 3-Kδ (IC50= 1.82, 0.07, and 1.24 for p110b, p110d, and p110g, respectively, but may also target p110a at concentrations as high as 100 µM with less potency) in NB-4 and primary APL cells. It has
been reported that the constitutive activation of PI3K/Akt signaling in primary AML cells is predominantly attributable
to PI 3-Kδ. Pharmacologic use of PI 3-Kδ inhibitor has been shown to block PI3K/Akt/mTOR signaling and could thereby
reduce proliferation and induce apoptosis. A related study further suggests PI 3-Kδ inhibitor as a key therapeutic target
among PI 3-K isoforms for allergy- and mast cell-related diseases.
 
Details
Chemical Formula:
 
C22H19N7O
CAS No.:
 
371242-69-2
Molecular weight:
 
397.44
Purity:
97% by HPLC
Appearance:
 
White solid
Chemical name:
 
 2-[6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
Solubility:
 
DMSO (5mg/mL)
Storage:
Protect from light. Packaged under inert gas
 
References
 
Product Name: LY 294002    PI3K Inhibitor
 
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A cell-permeable, potent, reversible and specific phosphatidylinositol 3-kinase inhibitor (IC50 = 1.4 µM) that acts on the
ATP-binding site of the enzyme. Also inhibits nonhomologous DNA end-joining (NHEJ) activity of the 460 kDa
phosphatidylinositol 3-like kinase DNA-PKcs, which is the catalytic subunit of DNA-activated protein kinase. Does not
affect the activities of EGF receptor kinase, MAP kinase, PKC, Pl 4-kinase, S6 kinase, and c-Src even at 50 µM. Blocks
the proliferation of cultured rabbit aortic smooth muscle cells without inducing apoptosis.
 
Details
Chemical Formula:
 
C19H17NO3
CAS No.:
 
154447-36-6
Molecular weight:
 
307.4
Purity:
99% by HPLC
Appearance:
 
Off-white solid
Chemical name:
 
 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
Solubility:
 
DMSO (20mg/mL) and ethanol (15mg/mL)
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Ordering informations
 
Catalog No.
Product Name
Size
CD0261
Compound 15e Dihydrochloride – PI3Ka Inhibitor
1mg, 5mg, 10mg
& 50mg
CD0245
GDC-0941 – PI3Ka/d Inhibitor
1mg, 5mg, 25mg, 50mg,
100mg, 200mg, 500mg & 1g
CD0278
17-b-Hydroxywortmannin (HWT)
1mg, 5mg, 10mg
& 25mg
CD0283
IC87114 - PI3Kδ Inhibitor
1mg, 5mg, 10mg, 25mg,
50mg, 100mg, 200mg & 1g
CD0342
LY 294002    PI3K Inhibitor
5mg, 10mg, 25mg, 50mg,
100mg, 200mg, 300mg & 1g
 
 
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