Size | Price | Stock | Qty |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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10g |
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50g |
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Other Sizes |
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Purity: ≥98%
Erlotinib mesylate (also known as OSI-744 mesylate, trade name: Tarceva) is the mesylate salt of erlotinib which is an EGFR (epidermal growth factor receptor) inhibitor with IC50 of 2 nM in cell-free assays, and is >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib is a quinazoline derivative with potent antineoplastic properties and has been approved for the treatment of non-small cell lung cancer (NSCLC), pancreatic cancer and several other types of cancer. It acts by competing with adenosine triphosphate and reversibly binding to the intracellular catalytic domain of EGFR tyrosine kinase, thereby reversibly inhibiting EGFR phosphorylation and blocking the signal transduction events and tumorigenic effects associated with EGFR activation.
ln Vitro |
With an IC50 of 1 nM, erlotinib mesylate (CP-358774 mesylate) is likewise a strong inhibitor of the EGFR's recombinant intracellular (kinase) domain. With an IC50 of 100 nM during an 8-day proliferation assay, erlotinib significantly inhibits the proliferation of DiFi cells[1]. When compared to either treatment alone, the combination of B-DIM with Erlotinib (2 μM) significantly inhibits the development of colonies in BxPC-3 cells. When compared to the apoptotic impact of either treatment alone, the combination of B-DIM and Erlotinib (2 μM) significantly induces apoptosis only in BxPC-3 cells[2].
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ln Vivo |
AUC0-inf following po treatment of Erlotinib (5 mg/kg) differs statistically significantly by 1.49 times between Bcrp1/Mdr1a/1b-/- and WT mice (7,419±1,720 versus 4,957±1,735 ng*h/mL, respectively, P=0.01)[3]. When Erlotinib (10 mg/kg/day or 20 mg/kg/day) is given to rats treated with Bleomycin (BLM), there is no evidence of a significant worsening of lung injuries as measured by indices such as lung weights, pulmonary hydroxyproline (HyP) level, histopathological scores (which include lung fibrosis score and lung lesion density), and scopic findings. According to the results, erlotinib does not worsen the pulmonary damage that BLM causes in rats[4].
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Animal Protocol |
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References |
[1]. Moyer JD, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997 Nov 1;57(21):4838-48.
[2]. Ali S, et al. Apoptosis-inducing effect of erlotinib is potentiated by 3,3'-diindolylmethane in vitro and in vivo using an orthotopic model of pancreatic cancer. Mol Cancer Ther, 2008, 7(6), 1708-1719. [3]. Marchetti S, et al. Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice.Mol Cancer Ther. 2008 Aug;7(8):2280-7. [4]. Adachi K, et al. Effects of erlotinib on lung injury induced by intratracheal administration of bleomycin (BLM) in rats. J Toxicol Sci. 2010 Aug;35(4):503-14 |
Molecular Formula |
C22H23N3O4.CH4O3S
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Molecular Weight |
489.541
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CAS # |
248594-19-6
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Related CAS # |
Erlotinib Hydrochloride;183319-69-9;Erlotinib;183321-74-6
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SMILES |
CS(=O)(O)=O.COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC
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Synonyms |
CP358774 mesylate; NSC 718781 mesylate;CP358774 mesylate, NSC 718781 mesylate;CP-358,774 mesylate; CP-358774 mesylate; OSI-774 mesylate; OSI 774 mesylate; OSI774 mesylate; Erlotinib mesylate
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0427 mL | 10.2137 mL | 20.4273 mL | |
5 mM | 0.4085 mL | 2.0427 mL | 4.0855 mL | |
10 mM | 0.2043 mL | 1.0214 mL | 2.0427 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.