ChemicalBook > CAS DataBase List > BEZ235 (Tosylate)

BEZ235 (Tosylate)

Product Name: BEZ235 (Tosylate)
CAS No.: 1028385-32-1
Chemical Name: BEZ235 (Tosylate)
Synonyms: BEZ235 (Tosylate);Dactolisib Tosylate;NVP-BEZ 235 Tosylate;BEZ235 p-toluene sulfonate;Dactolisib Tosylate, 10 mM in DMSO;DACTOLISIB TOSYLATE (BEZ235 TOSYLATE);NVP-BEZ 235 Tosylate (BEZ235 Tosylate);4-methylbenzenesulfonic acid,2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile;2-Methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)- phenyl]propionitrile p-toluenesulfonate salt;4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-alpha,alpha-dimethylbenzeneacetonitrile 4-methylbenzenesulfonate
CBNumber: CB92624096
Molecular Formula: C37H31N5O4S
Formula Weight: 641.75
MOL File: 1028385-32-1.mol

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BEZ235 (Tosylate) Property

storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: Powder
color: Off-white to light yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0711
Product name: DactolisibTosylate
Purity: 99.88%
Packaging: 50mg
Price: $72
Updated: 2021/12/16

ApexBio Technology

Product number: A3238
Product name: BEZ235Tosylate
Packaging: 100mg
Price: $92
Updated: 2021/12/16

ChemScene

Product number: CS-0711
Product name: DactolisibTosylate
Purity: 99.88%
Packaging: 100mg
Price: $108
Updated: 2021/12/16

ChemScene

Product number: CS-0711
Product name: DactolisibTosylate
Purity: 99.88%
Packaging: 200mg
Price: $180
Updated: 2021/12/16

ApexBio Technology

Product number: A3238
Product name: BEZ235Tosylate
Packaging: 500mg
Price: $294
Updated: 2021/12/16

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BEZ235 (Tosylate) Chemical Properties,Usage,Production

Uses

A dual ATP-competitive inhibitor of PI3K and mTOR. p110α, IC50=4 nM; p110β, IC50=75 nM; p110δ, IC50=7 nM; p110γ, IC50=5 nM.

Biological Activity

bez235 is an imidazoquinoline derivative inhibiting both pi3k and mtor kinases with low nanomolar ic50s. it was well tolerated in preclinical animal studies as well as in

in vivo

Dactolisib (BEZ235) is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, Dactolisib (BEZ235) appears rapidly in plasma with a C_max of 1.68 μM at 0.5 h and a C_24h of 0.03 μM^[1].

IC 50

p110α: 4 nM (IC₅₀); p110α-H1047R: 4.6 nM (IC₅₀); p110α-E545K: 5.7 nM (IC₅₀); p110γ: 5 nM (IC₅₀); p110δ: 7 nM (IC₅₀); p110β: 75 nM (IC₅₀); mTOR: 20.7 nM (IC₅₀); mTORC1; mTORC2; Autophagy

References

1. maira sm, stauffer f, brueggen j et al. identification and characterization of nvp-bez235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. mol cancer ther 2008; 7: 1851-1863.2. markman b, tabernero j, krop i et al. phase i safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mtor inhibitor bgt226 in patients with advanced solid tumors. ann oncol 2012; 23: 2399-2408.3. schnell cr, stauffer f, allegrini pr et al. effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor nvp-bez235 on the tumor vasculature: implications for clinical imaging. cancer res 2008; 68: 6598-6607.4. mukherjee b, tomimatsu n, amancherla k et al. the dual pi3k/mtor inhibitor nvp-bez235 is a potent inhibitor of atm- and dna-pkcs-mediated dna damage responses. neoplasia 2012; 14: 34-43.5. serra v, markman b, scaltriti m et al. nvp-bez235, a dual pi3k/mtor inhibitor, prevents pi3k signaling and inhibits the growth of cancer cells with activating pi3k mutations. cancer res 2008; 68: 8022-8030.

BEZ235 (Tosylate) Preparation Products And Raw materials

Raw materials

Preparation Products

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1028385-32-1, BEZ235 (Tosylate)Related Search:

Infigratinib NVP-BAW2881 NVP-AAM077 NVP-LDE225 NVP-TNKS656 TAE226 (NVP-TAE226) NVP-ADW742 NVP-CGM097 NVP-BEP800 NVP-TAE684 NVP-BEZ 235 Sodium p-toluenesulfonate

BEZ235 (Tosylate)

NVP-BEZ 235 Tosylate

4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-alpha,alpha-dimethylbenzeneacetonitrile 4-methylbenzenesulfonate

NVP-BEZ 235 Tosylate (BEZ235 Tosylate)

2-Methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)- phenyl]propionitrile p-toluenesulfonate salt

4-methylbenzenesulfonic acid,2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile

Dactolisib Tosylate

DACTOLISIB TOSYLATE (BEZ235 TOSYLATE)

BEZ235 p-toluene sulfonate

Dactolisib Tosylate, 10 mM in DMSO

1028385-32-1

C37H31N5O4S

C30H23N5OC7H8O3S