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작성일 : 14-01-20
[Chemdea] PI3K/mTOR Inhibitors (3)
BEZ235 - NVP-BEZ235 – PI3Ka/g/d Inhibitor / NVP-BEZ235 Hydrochloride - PI3Ka/g/d Inhibitor PI-103 – PI3K, mTOR and DNA-PK Inhibitor / PI-103 Hydrochloride – PI3K, mTOR and DNA-PK Inhibitor PIK-75 – PI3Ka Inhibitor VIII
PI3K/mTOR Inhibitors (3)
 
 
Product Name: BEZ235 - NVP-BEZ235 – PI3Ka/g/d Inhibitor
 
   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요
 
Potent, orally active dual PI3K/mTOR inhibitor under clinical trials. Inhibits PI3 kinase (PI3K), with p110α IC50 = 4 nM,
p110b IC50 =75 nM, p110d IC50 =7 nM, p110g IC50 =5 nM. BEZ235 showed high target specificity and demonstrated
antiproliferative activity against tumor cell lines in animal models.
 
Details
Chemical Formula:
 
C30H23N5O
CAS No.:
 
915019-65-7
Molecular weight:
 
469.5
Purity:
99% by HPLC
Appearance:
 
Off-White solid
Chemical name:
 
4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-a,a-
dimethylbenzeneacetonitrile
Solubility:
 
DMSO (2 mg/mL). The hydrochloride form of NVP-BEZ235 (Cat # CD0196) has 10-fold
higher solubility.
Storage:
Protect from light. Packaged under inert gas
 
Reference
 
 
Product Name: BEZ235 - NVP-BEZ235 Hydrochloride  - PI3Ka/g/d Inhibitor
 
   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요
 
Potent, orally active dual PI3K/mTOR inhibitor under clinical trials. Inhibits PI3 kinase (PI3K), with p110α IC50 = 4 nM,
p110b IC50 =75 nM, p110d IC50 =7 nM, p110g IC50 =5 nM. BEZ235 showed high target specificity and demonstrated
antiproliferative activity against tumor cell lines in animal models.
 
Details
Chemical Formula:
 
C30H23N5O
CAS No.:
 
915019-65-7
Molecular weight:
 
506.0
Purity:
98% by HPLC
Appearance:
 
Light yellow solid
Chemical name:
 
4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-a,a-
dimethylbenzeneacetonitrile hydrochloride
Solubility:
 
DMSO (20 mg/mL). Molecular Formula: C30H23N5O.
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Product Name: PI-103 – PI3K, mTOR and DNA-PK Inhibitor
 
   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요
 
A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP competitive inhibitor of DNA-PK, 
PI3-K, and mTOR (IC50; DNA-PK = 2 nM, p110a = 8 nM , p110b = 88 nM, p110d = 48 nM, p110g = 150 nM, PI3-KC2b =
26 nM, mTORC1 = 20 nM, and mTORC2 = 83 nM). It inhibits ATR and ATM only at much higher concentrations (IC50
850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at
concentrations as high as 10 µM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines
both in vitro and in vivo.
 
Details
Chemical Formula:
 
C19H16N4O3
CAS No.:
 
371935-74-9
Molecular weight:
 
348.4
Purity:
99% by HPLC
Appearance:
 
Off-White solid
Chemical name:
 
3-(4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl)phenol
Solubility:
 
DMSO (5 mg/mL; slight warming might be required to complete solubilization). A 6-fold more soluble hydrochloride salt of PI-103 is also available (Cat# CD0205). 
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Product Name: PI-103 Hydrochloride – PI3K, mTOR and DNA-PK Inhibitor
 
   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요
 
A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP competitive inhibitor of DNA-PK, 
PI3-K, and mTOR (IC50; DNA-PK = 2 nM, p110a = 8 nM , p110b = 88 nM, p110d = 48nM, p110g = 150 nM, PI3-KC2b =
26 nM,mTORC1 = 20 nM, and mTORC2 = 83 nM). It inhibits ATR and ATM only at much higher oncentrations (IC50
850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at
concentrations as high as 10 µM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines
both in vitro and in vivo.
 
Details
Chemical Formula:
 
C19H16N4O3*HCl.
CAS No.:
 
371935-79-4
Molecular weight:
 
384.8
Purity:
99% by HPLC
Appearance:
 
Off-White solid
Chemical name:
 
 3-(4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl)phenol Hydrochloride
Solubility:
 
DMSO (30 mg/mL). This hydrochloride salt form is 6-fold more soluble than the
corresponding free base (Cat# CD0113).
Storage:
Protect from light. Packaged under inert gas
 
References
 
Product Name: PIK-75 – PI3Ka Inhibitor VIII
 
   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요
 
A cell-permeable imidazopyridine compound that acts as a highly potent and ATP-competitive DNA-PK and p110α-
selective PI3-K inhibitor (IC50 = 7.8, 40, 100, and 850 nM for p110α, p110γ, PI 3-K C2β, and p110β, respectively). Shown
to effectively block cellular PI3-K/Akt signaling and inhibit tumor growth both in vitro (IC50 ≤58 nM in MCF7, MCF7
ADR-res, HeLa, A375, and A549 cultures) and in mice in vivo (62% inhibition of HeLa xenograft in 2 weeks, 50 mg/kg/
day, i.p.).
 
Details
Chemical Formula:
 
C16H14N5O4SBr•HCl•2H2O
CAS No.:
 
372196-67-3
Molecular weight:
 
524.8
Purity:
99% by HPLC
Appearance:
 
Pale yellow solid
Chemical name:
 
N-((1E)-(6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N′-methyl-N′′-(2-methyl-5-
nitrobenzene) sulfonohydrazide, HCl
Solubility:
 
DMSO (10 mg/mL)
Storage:
Protect from light. Packaged under inert gas
 
References
 
 
Ordering informations
 
Catalog No.
Product Name
Size
CD0195
BEZ235 - NVP-BEZ235 – PI3Ka/g/d Inhibitor
5mg, 10mg, 25mg, 50mg
& 100mg
CD0196
NVP-BEZ235 Hydrochloride  - PI3Ka/g/d Inhibitor
5mg, 10mg, 25mg, 50mg
& 100mg
CD0113
PI-103 – PI3K, mTOR and DNA-PK Inhibitor
1mg, 5mg, 10mg, 25mg, 50mg,
100mg, 250mg & 1g
CD0205
PI-103 Hydrochloride – PI3K, mTOR and DNA-PK Inhibitor
1mg, 5mg, 10mg, 25mg,
50mg & 100mg
CD0273
PIK-75 – PI3Ka Inhibitor VIII
1mg, 5mg, 10mg, 25mg,
50mg, 100mg, 200mg & 1g
 
 
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