| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
KRASG12D-IN-7 (Compound (R)-5a) (72 hours) showed potent and selective antiproliferative activity against AsPC-1 cells (IC50 = 10 nM), GP2D cells (IC50 = 2.7 nM), AGS cells (IC50 = 6.1 nM), HPAF-II cells (IC50 = 6.8 nM) and Ls513 cells (IC50 = 27.3 nM) carrying the KRASG12D mutation, while having no significant inhibitory effect on other KRAS mutants (H358 G12C, G12S) and KRAS wild-type cell lines (IC50 > 1000 nM)[1]. KRASG12D-IN-7 can bind to both GDP- and GTP-bound KRASG12D, selectively inhibiting the interaction between GDP-bound KRASG12D and SOS1, and blocking the binding of GTP-bound KRASG12D to RAF1 [1]. KRASG12D-IN-7 (1-1000 nM, 3 hours) dose-dependently reduced the protein levels of p-ERK and p-S6 in AsPC-1 cells, effectively inhibiting the downstream MAPK signaling pathway of KRAS [1]. KRASG12D-IN-7 (1-1000 nM, 24-72 hours) induced G0/G1 phase arrest and apoptosis in AsPC-1 cells [1]. KRASG12D-IN-7 (5 nM, 10 days) strongly inhibited colony formation in AsPC-1 cells [1].
|
|---|---|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: AsPC-1 cells Tested Concentrations: 1, 10, 100, 1000 nM Incubation Duration: 3 h Experimental Results: Reduced the protein levels of p-ERK and p-S6 in AsPC-1 cells. Cell Cycle Analysis[1] Cell Types: AsPC-1 cells Tested Concentrations: 1, 10, 100, 1000 nM Incubation Duration: 24 h Experimental Results: Increased G0/G1 phase cell proportion. Downregulated CDK2/Cyclin D3 protein levels. Apoptosis Analysis[1] Cell Types: AsPC-1 cells Tested Concentrations: 1, 10, 100, 1000 nM Incubation Duration: 72 h Experimental Results: Induced apoptosis in AsPC-1 cells. Increased Annexin V-positive cells. Upregulated cPARP/cCasp-3 protein levels. |
| References |
| Molecular Formula |
C31H32CLF2N7OSE
|
|---|---|
| Molecular Weight |
671.04
|
| Appearance |
Typically exists as solids at room temperature
|
| 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 | 1.4902 mL | 7.4511 mL | 14.9022 mL | |
| 5 mM | 0.2980 mL | 1.4902 mL | 2.9804 mL | |
| 10 mM | 0.1490 mL | 0.7451 mL | 1.4902 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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