| Size | Price | Stock | Qty |
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| 10mg |
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| Other Sizes |
| Targets |
(R)-BI-2852 is an inactive isomer and does not have significant biological activity. It serves as a negative control in experiments where BI-2852 is the active KRAS inhibitor. The active compound targets KRAS, a key oncogene involved in numerous cancers.
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|---|---|
| ln Vitro |
As an inactive control compound, (R)-BI-2852 does not exhibit significant KRAS inhibitory activity. It is used to validate that observed effects in experiments are due to the active compound rather than non-specific effects. It shows no antiproliferative or antitumor activity in standard assays.
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| ln Vivo |
In vivo, (R)-BI-2852 is not expected to exhibit pharmacological activity. It may be used as a negative control in animal studies to distinguish the effects of the active compound from non-specific effects. Its lack of activity makes it a valuable tool for validating experimental results in KRAS research.
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| Enzyme Assay |
Cell-free enzyme assays for (R)-BI-2852: KRAS binding affinity is measured using surface plasmon resonance or fluorescence polarization assays. The compound is incubated with KRAS protein and binding is measured. The inactive enantiomer should show no significant binding. GTPase activity or nucleotide exchange assays can also be used to assess functional inhibition.
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| Cell Assay |
Cellular assays for (R)-BI-2852: KRAS-mutant cancer cells (e.g., HCT116, A549) are treated with (R)-BI-2852 as a control alongside the active compound. Cell proliferation is measured by MTT or colony formation assays. KRAS downstream signaling (e.g., ERK, AKT phosphorylation) is assessed by Western blot. The inactive enantiomer should show no effect on cell growth or signaling.
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| Animal Protocol |
In vivo animal studies for (R)-BI-2852: xenograft mouse models of KRAS-mutant cancers are used. Mice are administered (R)-BI-2852 as a control group in efficacy studies. Tumor growth, signaling pathway modulation, and toxicity are compared between active and control groups to validate the therapeutic effects of BI-2852.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (R)-BI-2852 are expected to be similar to those of BI-2852, as they are enantiomers. As a small molecule (molecular weight 516.59), it may have moderate oral bioavailability and tissue distribution. It is likely metabolized in the liver and excreted via the kidneys. Detailed PK data are limited.
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| Toxicity/Toxicokinetics |
Toxicity of (R)-BI-2852: as an inactive isomer used as a control compound, it is expected to have low toxicity. No specific toxicity data are available. It is for research use only and not intended for human therapeutic applications. Standard laboratory safety precautions should be followed during handling.
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| References | |
| Additional Infomation |
(R)-BI-2852 is a research-grade compound used as an experimental control in KRAS inhibitor research. Its primary application is to validate the specificity and activity of BI-2852. It is not a therapeutic agent and has no clinical applications. It is available as a reference standard for analytical and pharmacological studies.
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| Molecular Formula |
C31H28N6O2
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|---|---|
| Molecular Weight |
516.593026161194
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| Exact Mass |
516.227
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| CAS # |
2375482-49-6
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| Related CAS # |
BI-2852;2375482-51-0
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| PubChem CID |
146167995
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
39
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| Complexity |
874
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1C=C(N=C1)CN2C=CC3=C2C=C(C=C3)CNCC4=C(C5=CC=CC=C5N4)[C@H]6C7=C(C=CC(=C7)O)C(=O)N6
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| InChi Key |
JYEQLXOWWLNVDX-SSEXGKCCSA-N
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| InChi Code |
InChI=1S/C31H28N6O2/c1-36-16-21(33-18-36)17-37-11-10-20-7-6-19(12-28(20)37)14-32-15-27-29(24-4-2-3-5-26(24)34-27)30-25-13-22(38)8-9-23(25)31(39)35-30/h2-13,16,18,30,32,34,38H,14-15,17H2,1H3,(H,35,39)/t30-/m1/s1
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| Chemical Name |
(3R)-5-hydroxy-3-[2-[[[1-[(1-methylimidazol-4-yl)methyl]indol-6-yl]methylamino]methyl]-1H-indol-3-yl]-2,3-dihydroisoindol-1-one
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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 (e.g. under nitrogen), 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) |
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 | 1.9358 mL | 9.6789 mL | 19.3577 mL | |
| 5 mM | 0.3872 mL | 1.9358 mL | 3.8715 mL | |
| 10 mM | 0.1936 mL | 0.9679 mL | 1.9358 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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