| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ALK-IN-22 (compound I-24) (72 hours) exhibits IC50 values of 11, 37, and 27 nM, respectively, demonstrating antiproliferative action against ALK-positive karpas299, H2228, and H3122 cell lines [1]. ALK-IN-22 (Compound I-24) suppresses downstream signal transducers AKT and ERK as well as ALK (0-100 nM; 24 hours; H2228 cells) [1]. Inducing apoptosis and achieving cell cycle arrest in the G1 phase, ALK-IN-22 (Compound I-24) (0-100 nM; 48 hours; H2228 cells) [1].
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| ln Vivo |
In vivo antitumor efficaciousness of ALK-IN-22 (Compound I-24) (25-50 mg/kg; ir; twice daily for 14 days) has been reported [1]. The Cmax and t1/2 values of ALK-IN-22 (Compound I-24) (10 mg/kg; oral) are 345.7 ng/mL and 4.1 hours, respectively [1]. The CL and t1/2 values of ALK-IN-22 (Compound I-24) (2 mg/kg; iv) are 36.2 mL/min/kg and 2.5 hours, respectively [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: H2228 Cell Tested Concentrations: 0, 25, 50 and 100 nM Incubation Duration: 24 hrs (hours) Experimental Results: Down-regulates ALK phosphorylation level, blocks the expression and activation of AKT and ERK, the key downstream signals of ALK. Dependency is formed. Apoptosis analysis [1] Cell Types: H2228 Cell Tested Concentrations: 0, 25, 50, 100 nM Incubation Duration: 48 hrs (hours) Experimental Results: At concentrations of 25 nM, 50 nM, and 100 nM, the cell apoptosis rates were 14.23% and 23.94 respectively. %, 31.70%, respectively. Cell cycle analysis [1] Cell Types: H2228 cells Tested Concentrations: 0, 25, 50 and 100 nM Incubation Duration: 48 hrs (hours) Experimental Results: The percentage of cells in G1 phase increased from 49.72% to 58.51% in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice [1]
Doses: 25 and 50 mg/kg Route of Administration: gavage; twice a day for 14 days. Experimental Results: The tumor growth inhibition (TGI) value of 50 mg/kg reached 93.5%. Animal/Disease Models: SD rat[1] Doses: 2 and 10 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: oral and intravenous (iv) (iv)injection Experimental Results:1.19 Parameter F16 VP-16 Dose (iv) mg/kg 10 10 Cmax (ng/mL) 26952 17712 Tmax (min) 5 5 AUC Plasma (min*ng/mL) 2878363 409528 T1/2 (min) 151 45 Vd (L/Kg) 0.2341 0.432 CL (L/min/kg) 0.001 0.007 |
| References |
| Molecular Formula |
C24H24CLN7O2
|
|---|---|
| Molecular Weight |
477.946063041687
|
| Exact Mass |
477.168
|
| CAS # |
2468219-09-0
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| PubChem CID |
154640729
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
4.4
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
34
|
| Complexity |
725
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NQJLJKFROUEMTA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H24ClN7O2/c1-13-20(23(34)32(3)4)15-10-9-14(11-19(15)28-13)29-24-27-12-17(25)21(31-24)30-18-8-6-5-7-16(18)22(33)26-2/h5-12,28H,1-4H3,(H,26,33)(H2,27,29,30,31)
|
| Chemical Name |
6-[[5-chloro-4-[2-(methylcarbamoyl)anilino]pyrimidin-2-yl]amino]-N,N,2-trimethyl-1H-indole-3-carboxamide
|
| HS Tariff Code |
2934.99.9001
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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)
|
| 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 | 2.0923 mL | 10.4613 mL | 20.9227 mL | |
| 5 mM | 0.4185 mL | 2.0923 mL | 4.1845 mL | |
| 10 mM | 0.2092 mL | 1.0461 mL | 2.0923 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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