| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Ceritinib also inhibits RET (IC50=400 nM), FGFR3 (IC50=430 nM), LCK (IC50=560 nM), JAK2 (IC50=610 nM), Aurora (IC50=660 nM), LYN (IC50=840 nM), EGFR (IC50=900 nM) and FGFR4 (IC50=950 nM) [1]. Ceritinib has a high inhibitory activity against ALK enzyme activity, with an IC50 value of 200 pM. Among 46 kinases, it showed strong inhibitory effects only against IGF-1R, InsR and STK22D, with a selectivity of at least 70-fold. In Ba/F3 cells transfected with multiple kinases, the IC50 value of ceritinib against ALK activity was 40.7 nM, and the IC50 values for all other tested kinases were greater than 100 nM. Ceritinib showed potent antiproliferative activity in Karpas 299 human non-Hodgkin Ki-positive large cell lymphoma cells carrying the NPM-ALK fusion gene, with an IC50 value of 22.8 nM; in Ba/F3 cells transfected with the NPM-ALK fusion gene, the IC50 value was 26 nM. Ceritinib also showed good selectivity against wild-type Ba/F3 cells (IC50>2 μM) and Ba/F3 cells transfected with the Tel-InsR gene (IC50=320 nM) [2].
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|---|---|
| ln Vivo |
Ceritinib has excellent pharmacokinetic characteristics in both rodents and non-rodents, with oral bioavailability >50%. Ceritinib exhibits dose-dependent tumor growth inhibition. In the Karpas 299 rat xenograft model, daily administration can cause partial tumor regression; while in the H2228 non-small cell lung cancer rat xenograft model carrying the EML4-ALK fusion gene, ceritinib can cause complete tumor regression. In both models, the animals tolerated ceritinib well. The ADME properties of ceritinib were further evaluated, and the results showed that it has relatively good metabolic stability in liver microsomes, moderate inhibitory effect on CYP3A4, and certain inhibitory effect on hERG channels in hERG patch-clamp experiments (IC50 value of 46 μM). However, no QTc interval prolongation was found in telemetry studies in dogs and monkeys [2].
|
| References |
|
| Molecular Formula |
C30H44CLN5O9S3
|
|---|---|
| Molecular Weight |
750.35
|
| CAS # |
2055376-74-2
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3.CS(=O)(O)=O.CS(=O)(O)=O
|
| Synonyms |
LDK378 mesylate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.3327 mL | 6.6636 mL | 13.3271 mL | |
| 5 mM | 0.2665 mL | 1.3327 mL | 2.6654 mL | |
| 10 mM | 0.1333 mL | 0.6664 mL | 1.3327 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.
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