| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
KRASG12C[1].
AZD4747 targets the mutant GTPase KRAS G12C, a common oncogenic driver in various cancers. It is a selective and potent inhibitor that binds to the mutant form of KRAS, locking it in an inactive GDP-bound state and preventing downstream signaling. |
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| ln Vitro |
In vitro, AZD4747 is a selective and potent inhibitor of KRAS G12C. It has potential antitumor activity and is being studied for its effects on KRAS G12C-mutated cancer cells.
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| ln Vivo |
In vivo, AZD4747 has potential antitumor activity in models of KRAS G12C-mutated cancers. Its ability to cross the blood-brain barrier makes it particularly relevant for the study of brain metastases or primary brain tumors with KRAS G12C mutations.
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| Enzyme Assay |
Non-cellular enzyme assays for AZD4747 involve measuring its inhibitory activity against KRAS G12C. The compound is incubated with the mutant KRAS protein and its substrates, and the inhibition of GTPase activity or downstream signaling is quantified.
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| Cell Assay |
In vitro cellular assays for AZD4747 are performed using KRAS G12C-mutated cancer cell lines. Cells are treated with the compound, and cell proliferation, signaling pathway inhibition, and induction of apoptosis are assessed.
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| Animal Protocol |
In vivo animal experiments for AZD4747 would typically be conducted in mouse xenograft models using KRAS G12C-mutated cancer cell lines. The compound is administered orally due to its oral activity, and tumor growth inhibition is the primary endpoint.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties: AZD4747 is orally active and is blood-brain barrier permeable. Detailed PK parameters such as half-life, Cmax, and AUC are not detailed in available sources but would be characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
Toxicological data for AZD4747 are not provided in available sources. As an investigational compound, its safety profile would be evaluated in preclinical toxicology studies.
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| References | |
| Additional Infomation |
AZD4747 is a selective, BBB-permeable inhibitor of KRAS G12C with potential antitumor activity. Its CAS number is 2489226-14-2. It is being studied for pancreatic and colorectal adenocarcinoma. No clinical trial or regulatory approval information is available.
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| Molecular Formula |
C24H22CLFN2O3
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|---|---|
| Molecular Weight |
440.89
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| CAS # |
2489226-14-2
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| Appearance |
White to off-white solid powder
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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 |
| 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) |
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
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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 | 2.2681 mL | 11.3407 mL | 22.6814 mL | |
| 5 mM | 0.4536 mL | 2.2681 mL | 4.5363 mL | |
| 10 mM | 0.2268 mL | 1.1341 mL | 2.2681 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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