| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
K-RAS
|
|---|---|
| ln Vitro |
Compound 9d, also known as 4S-PROTAC SOS1 degrader-1, exhibits strong SOSI degradation activity in NCI-H358 cells, with SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM, respectively[1]. In NCI-H358 cells, SOS1 is degraded in a dose- and time-dependent manner by (4S)-PROTAC SOS1 degrader-1 (24 h)[1]. In NCI-H358 cells, (4S)-PROTAC SOS1 degrader-1 (9.8-2500 nM; 24 h) does not cause SOS2 and KRAS degradation[1]. In NCI-H358 cells, (4S)-PROTAC SOS1 degrader-1 (7.8-2000 nM; 24 h) reduces pERK expression and RAS-GTP level in a dose-dependent manner[1].
|
| ln Vivo |
With an excellent safety profile, PROTAC SOS1 degrader-2 (10, 20 mg/kg; ip, daily for 21 days) effectively reduces the growth of tumors in vivo[1].
|
| Animal Protocol |
Animal/Disease Models: BALB/c nude mice (NCI-H358 tumor xenografts )[1]
Doses: 10, 20 mg/kg Route of Administration: IP; daily, 21 days Experimental Results: Dramatically inhibited the tumor growth in vivo with a good safety profile. |
| References |
| Molecular Formula |
C57H76CLFN10O4S
|
|---|---|
| Molecular Weight |
1051.79
|
| CAS # |
2913176-81-3
|
| Related CAS # |
PROTAC SOS1 degrader-1;2913185-35-8
|
| Appearance |
Typically exists as solid 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 | 0.9508 mL | 4.7538 mL | 9.5076 mL | |
| 5 mM | 0.1902 mL | 0.9508 mL | 1.9015 mL | |
| 10 mM | 0.0951 mL | 0.4754 mL | 0.9508 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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