| Size | Price | |
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| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| ln Vitro |
Compound 10zi, or Ack1 inhibitor 1, has an IC50 of 3.71 μM for 67R cells and 4.18 μM for H1975 cells, respectively, which inhibits cell growth [1]. When used alone or in conjunction with ASK120067, Ack1 inhibitor 1 (0 nM-5000 nM, 72 h) can improve the anti-tumor effect in 67R cells [1]. The phosphorylation of ACK1 and AKT in 67R cells is dose-dependently inhibited by Ack1 inhibitor 1 (1 μM and 5 μM, 6 h) [1].
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| ln Vivo |
In SD rats, a single oral dose of 10 mg/kg of Ack1 inhibitor 1 (Compound 10zi) improves the AUC value of 1920.56 h•ng/mL, Cmax of 119.52 μg/L, and oral bioavailability of 19.80%[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: 67R cells (ASK120067-resistant cells obtained from parental H1975 cells by a dose escalation method). Tested Concentrations: 0-5000 nM (combined with ASK120067) Incubation Duration: 72 h Experimental Results: Caused strong synergistic anti -growth effects on 67R cells with high synergy scores of 10.83, respectively Western Blot Analysis[1] Cell Types: 67R cells Tested Concentrations: 1 μM and 5 μM Incubation Duration: 6 h (stimulated with or without EGF for 30 min) Experimental Results: Caused moderate down-regulation of p-ACK1 and p-AKT at 1 μM. demonstrated better potency against p-AKT, while it was unable to completely inhibit p-ACK1 at 5 μM. |
| References |
[1]. Li Q, et al. Design, Synthesis, and Evaluation of (R)-8-((Tetrahydrofuran-2-yl)methyl)pyrido[2,3-d]pyrimidin-7-ones as Novel Selective ACK1 Inhibitors to Combat Acquired Resistance to the Third-Generation EGFR Inhibitor. J Med Chem. 2023 May 25;66(10):6905-6921.
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| Molecular Formula |
C39H40F3N7O4
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|---|---|
| Molecular Weight |
727.77
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| CAS # |
2924415-92-7
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3741 mL | 6.8703 mL | 13.7406 mL | |
| 5 mM | 0.2748 mL | 1.3741 mL | 2.7481 mL | |
| 10 mM | 0.1374 mL | 0.6870 mL | 1.3741 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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