Dactolisib tosylate
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MedKoo CAT#: 581211

CAS#: 1028385-32-1 (tosylate)

Description: Dactolisib tosylate is also known as NVP-BEZ 235 Tosylate. NVP-BEZ235 is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. The IC50s for PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of NVP-BEZ235, with an average GI50 of 10 to 12 nM. In Vivo NVP-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, NVP-BEZ235 appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM.


Chemical Structure

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Dactolisib tosylate
CAS# 1028385-32-1 (tosylate)

Theoretical Analysis

MedKoo Cat#: 581211
Name: Dactolisib tosylate
CAS#: 1028385-32-1 (tosylate)
Chemical Formula: C37H31N5O4S
Exact Mass: 641.2097
Molecular Weight: 641.75
Elemental Analysis: C, 69.25; H, 4.87; N, 10.91; O, 9.97; S, 5.00

Price and Availability

Size Price Availability Quantity
100.0mg USD 350.0 2 Weeks
200.0mg USD 550.0 2 Weeks
500.0mg USD 950.0 2 Weeks
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Related CAS #: 1028385-32-1 (tosylate)   915019-65-7 (free base)    

Synonym: Dactolisib tosylate; NVP-BEZ235-ANA; UNII-U54GT9151S; BEZ235 Tosylate; NVP-BEZ 235 Tosylate;

IUPAC/Chemical Name: 2-Methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo(4,5-c)quinolin-1-yl)phenyl)propanenitrile 4-methylbenzenesulfonate

InChi Key: FWURTHAUPVXZHW-UHFFFAOYSA-N

InChi Code: InChI=1S/C30H23N5O.C7H8O3S/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36;1-6-2-4-7(5-3-6)11(8,9)10/h4-17H,1-3H3;2-5H,1H3,(H,8,9,10)

SMILES Code: CC(C1=CC=C(N(C2=C3C=NC4=CC=C(C5=CC6=CC=CC=C6N=C5)C=C24)C(N3C)=O)C=C1)(C)C#N.O=S(C7=CC=C(C)C=C7)(O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 641.75 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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