PI3K/mTOR Inhibitors (2)
본문
PI3K/mTOR Inhibitors (2)
Product Name: Compound 15e Dihydrochloride – PI3Ka Inhibitor
|
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
|
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)
|
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
|
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
|
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
|
댓글목록
등록된 댓글이 없습니다.