PI3K/mTOR Inhibitors (3)
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PI3K/mTOR Inhibitors (3)
Product Name: BEZ235 - NVP-BEZ235 – PI3Ka/g/d Inhibitor
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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.
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Details
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Chemical Formula:
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C30H23N5O
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CAS No.:
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915019-65-7
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Molecular weight:
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469.5
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Purity:
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99% by HPLC
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Appearance:
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Off-White solid
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Chemical name:
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4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-a,a- dimethylbenzeneacetonitrile
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Solubility:
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higher solubility.
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Storage:
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Protect from light. Packaged under inert gas
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Reference
Product Name: BEZ235 - NVP-BEZ235 Hydrochloride - PI3Ka/g/d Inhibitor
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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.
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Details
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Chemical Formula:
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C30H23N5O
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CAS No.:
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915019-65-7
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Molecular weight:
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506.0
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Purity:
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98% by HPLC
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Appearance:
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Light yellow solid
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Chemical name:
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4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-a,a- dimethylbenzeneacetonitrile hydrochloride
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Solubility:
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DMSO (20 mg/mL). Molecular Formula: C30H23N5O.
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Storage:
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Protect from light. Packaged under inert gas
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References
Product Name: PI-103 – PI3K, mTOR and DNA-PK Inhibitor
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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.
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Details
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Chemical Formula:
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C19H16N4O3
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CAS No.:
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371935-74-9
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Molecular weight:
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348.4
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Purity:
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99% by HPLC
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Appearance:
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Off-White solid
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Chemical name:
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3-(4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl)phenol
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Solubility:
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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).
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Storage:
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Protect from light. Packaged under inert gas
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References
Product Name: PI-103 Hydrochloride – PI3K, mTOR and DNA-PK Inhibitor
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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 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.
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Details
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Chemical Formula:
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C19H16N4O3*HCl.
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CAS No.:
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371935-79-4
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Molecular weight:
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384.8
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Purity:
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99% by HPLC
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Appearance:
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Off-White solid
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Chemical name:
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3-(4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl)phenol Hydrochloride
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Solubility:
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DMSO (30 mg/mL). This hydrochloride salt form is 6-fold more soluble than the
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Storage:
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Protect from light. Packaged under inert gas
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References
Product Name: PIK-75 – PI3Ka Inhibitor VIII
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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.).
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Details
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Chemical Formula:
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C16H14N5O4SBr•HCl•2H2O
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CAS No.:
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372196-67-3
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Molecular weight:
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524.8
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Purity:
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99% by HPLC
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Appearance:
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Pale yellow solid
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Chemical name:
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N-((1E)-(6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N′-methyl-N′′-(2-methyl-5- nitrobenzene) sulfonohydrazide, HCl
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Solubility:
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DMSO (10 mg/mL)
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Storage:
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Protect from light. Packaged under inert gas
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References
Ordering informations
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Catalog No.
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Product Name
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Size
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CD0195
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BEZ235 - NVP-BEZ235 – PI3Ka/g/d Inhibitor
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5mg, 10mg, 25mg, 50mg
& 100mg
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CD0196
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NVP-BEZ235 Hydrochloride - PI3Ka/g/d Inhibitor
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5mg, 10mg, 25mg, 50mg
& 100mg
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CD0113
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PI-103 – PI3K, mTOR and DNA-PK Inhibitor
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1mg, 5mg, 10mg, 25mg, 50mg,
100mg, 250mg & 1g
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CD0205
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PI-103 Hydrochloride – PI3K, mTOR and DNA-PK Inhibitor
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1mg, 5mg, 10mg, 25mg,
50mg & 100mg
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CD0273
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PIK-75 – PI3Ka Inhibitor VIII
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1mg, 5mg, 10mg, 25mg,
50mg, 100mg, 200mg & 1g
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