Size | Price | Stock | Qty |
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1mg |
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Other Sizes |
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ln Vitro |
SIAIS164018 hydrochloride (0–1 μM; 16 hours) strongly suppresses the growth of SR cells [1]. In 293T overexpressing ALK(G1202R) and H1975 cell lines expressing EGFR, SIAIS164018 (0-100 nM; 72 h) hydrochloride demonstrated superior cell growth inhibition than Brigatinib [1]. Significant G1 cell cycle arrest is induced in ALK-negative Calu-1 and MDA-MB-231 cells by SIAIS164018 (100 nM; 24 or 48 hours) hydrochloride [1]. ALK-positive SR cell lines and ALK-negative Calu-1 cell lines exhibit decreased protein levels of FAK, PYK2, FER, RSK1, and GAK when exposed to SIAIS164018 (0.01-1000 nM; 16 hours) hydrochloride [1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: SR cells Tested Concentrations: 0-1 μM Incubation Duration: 16 h Experimental Results: Dramatically inhibited SR cell proliferation with an IC50 value of 2 nM. Cell Proliferation Assay[1] Cell Types: ALK(G1202R) over-expressing 293T and EGFR expressing H1975 cell lines Tested Concentrations: 0-100 nM Incubation Duration: 72 h Experimental Results: demonstrated better cell proliferation inhibition than Brigatinib does in ALK(G1202R) over-expressing 293T and EGFR expressing H1975 cell lines with IC50s 21 and 42 nM, respectively. Cell Cycle Analysis[1] Cell Types: ALK-negative Calu-1 and MDA-MB-231 cells Tested Concentrations: 100 nM Incubation Duration: 24 or 48 h Experimental Results: Induced a significant G1 cell cycle arrest in ALK- negative Calu-1 and MDA-MB-231 cells. Western Blot Analysis[1] Cell Types: SR and Calu-1 cells Tested Concentrations: 0.01, 0.1, 1, 10, 100 and 1000 nM Incubation Duration: 16 h Experimental Results: Down- Regulates the protein level of FAK, PYK2, FER, RSK1, and GAK. |
References |
[1]. Ren C, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. J Med Chem. 2021 Jul 8;64(13):9152-9165.
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Molecular Formula |
C43H49CL2N10O7P
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Molecular Weight |
919.79
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Related CAS # |
SIAIS164018;2353492-68-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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) |
DMSO :~75 mg/mL (~81.54 mM)
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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 | 1.0872 mL | 5.4360 mL | 10.8720 mL | |
5 mM | 0.2174 mL | 1.0872 mL | 2.1744 mL | |
10 mM | 0.1087 mL | 0.5436 mL | 1.0872 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.