| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
H3122, H2228, Karpas299, and A549 are all significantly inhibited by ALK-IN-23 (compound Y28) (0–5 μM; 72h)[1]. H2228 cell colonies are obviously reduced by ALK-IN-23 (25–100 nM; 3 days), and at 100 nM, colony formation is nearly entirely eliminated[1]. H2228 cell apoptosis is accelerated by ALK-IN-23 (100–200 nM; 48 h)[1]. At a concentration of 10 nM, it is efficient to inhibit the migration of most cells (5-10 nM; 24 and 48 h)[1]. The percentage of cells in the G2 phase is dramatically increased by ALK-IN-23 (25–100 nM; overnight)[1].
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|---|---|
| ln Vivo |
Rats with ALK-IN-23 have a high intrinsic liver clearance of 152.9 mL/min/kg and a moderate half-life of 16.3 min[1]. In an H2228 xenograft mouse model, ALK-IN-23 (25 and 50 mg/kg; IG; once every 2 days; for 14 days) showed modest antitumor efficacy and no appreciable weight loss[1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: H3122, H2228, Karpas299 and A549 Tested Concentrations: 0-5 μM Incubation Duration: 72 h Experimental Results: demonstrated highly inhibitory activity against H3122, H2228, Karpas299 and A549 with IC50s of 12 nM, 17 nM, 15 nM and 1.33 μM. Apoptosis Analysis[1] Cell Types: H2228 cells Tested Concentrations: 100 nM, 200 nM Incubation Duration: 48 h Experimental Results: Facilitated the apoptosis of H2228 cells in a dose dependent manner and demonstrated a more pro-apoptotic effect than that of Ceritinib. Cell Migration Assay [1] Cell Types: H2228 cells Tested Concentrations: 5 nM and 10 nM Incubation Duration: 24 and 48 h Experimental Results: Blocked the migration of most cells at a dose of 10 nM (migration rate: 24 h 2.31%, 48 h: 5.01%). Cell Cycle Analysis[1] Cell Types: H2228 cells Tested Concentrations: 25 nM, 50 nM, 100 nM Incubation Duration: Overnight Experimental Results: Dramatically increased the percentage of cells in the G2 phase from 11.28% to 73.23% in a dramatic dose-dependent manner, accompanied by a resultant loss of G1-and S-phase populatio |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice (5×106 cells H2228 cells suspended in serum-free media were injected into the flanks)[1]
Doses: 25 and 50 mg/kg Route of Administration: IG; once every 2 days; for 14 days Experimental Results: Presented moderate antitumor efficacy with the tumor growth inhibition (TGI) of 70.46% at 50 mg/kg. Possessed gentle antitumor efficacy and demonstrated no significant weight loss. |
| References |
| Molecular Formula |
C26H29CLN8O3S
|
|---|---|
| Molecular Weight |
569.08
|
| Exact Mass |
568.177
|
| CAS # |
3033549-18-4
|
| PubChem CID |
165412707
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
4
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
39
|
| Complexity |
931
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=CC4=C(C=C3)C(=NN4)NC(=O)CN5CCCC5
|
| InChi Key |
YTTYYCAUZAPRNY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H29ClN8O3S/c1-16(2)39(37,38)22-8-4-3-7-20(22)30-25-19(27)14-28-26(32-25)29-17-9-10-18-21(13-17)33-34-24(18)31-23(36)15-35-11-5-6-12-35/h3-4,7-10,13-14,16H,5-6,11-12,15H2,1-2H3,(H2,28,29,30,32)(H2,31,33,34,36)
|
| Chemical Name |
N-[6-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-1H-indazol-3-yl]-2-pyrrolidin-1-ylacetamide
|
| 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
|
|---|---|
| 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 | 1.7572 mL | 8.7861 mL | 17.5722 mL | |
| 5 mM | 0.3514 mL | 1.7572 mL | 3.5144 mL | |
| 10 mM | 0.1757 mL | 0.8786 mL | 1.7572 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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