| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| Other Sizes |
| Targets |
CBFβ-RUNX1 inhibitor 1 targets the CBFβ-RUNX1 protein complex, which is a critical transcription factor complex involved in hematopoiesis and leukemogenesis. Chromosomal translocations involving the RUNX1 gene are associated with acute myeloid leukemia (AML) and other hematological malignancies. By inhibiting the CBFβ-RUNX1 interaction, the compound may disrupt RUNX1-mediated transcription and have therapeutic potential for leukemia.
|
|---|---|
| ln Vitro |
In vitro activity data for CBFβ-RUNX1 inhibitor 1 have not been reported in the available public literature. As a research compound targeting the CBFβ-RUNX1 protein-protein interaction, it may have been evaluated in biochemical and cell-based assays for its ability to disrupt this interaction and inhibit leukemia cell growth. Specific IC50 values and other activity parameters would be available from the primary literature.
|
| ln Vivo |
In vivo efficacy data for CBFβ-RUNX1 inhibitor 1 have not been reported in the available public literature. The compound may have been evaluated in animal models of leukemia depending on its research application. Specific information on dosing, efficacy, and pharmacodynamic effects would be available from the primary literature.
|
| Enzyme Assay |
For in vitro protein-protein interaction assays, recombinant CBFβ and RUNX1 proteins are incubated with labeled or unlabeled CBFβ-RUNX1 inhibitor 1 at various concentrations. Binding affinity and inhibition of complex formation are measured using techniques such as fluorescence polarization, AlphaScreen, or surface plasmon resonance.
|
| Cell Assay |
For cell-based assays, leukemia cell lines dependent on CBFβ-RUNX1 function are treated with CBFβ-RUNX1 inhibitor 1 at various concentrations. Cell viability and proliferation are measured using MTT or CellTiter-Glo assays. RUNX1 target gene expression is assessed by qRT-PCR to confirm inhibition of the CBFβ-RUNX1 complex.
|
| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice would be implanted with leukemia xenografts. When tumors reach a predetermined size, mice would be randomized and treated with CBFβ-RUNX1 inhibitor 1 via appropriate routes at doses determined from pharmacokinetic studies. Tumor volumes and leukemia burden would be assessed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of CBFβ-RUNX1 inhibitor 1 have not been characterized in the available public literature. Standard PK studies including oral bioavailability, half-life, protein binding, and tissue distribution would be required for in vivo studies. The compound is for research use only and is not intended for human or veterinary use.
|
| Toxicity/Toxicokinetics |
Toxicological data for CBFβ-RUNX1 inhibitor 1 have not been reported in the available public literature. As a research compound, it is intended for laboratory use only and is not for human or veterinary use. Standard safety precautions should be followed when handling this compound. Comprehensive toxicology studies would be required before any clinical development.
|
| References |
:PCT Int. Appl. (2019), WO 201909959
|
| Additional Infomation |
CBFβ-RUNX1 inhibitor 1 is a research compound (CAS 2328140-37-8) targeting the CBFβ-RUNX1 protein-protein interaction. Comprehensive information regarding its target, activity, pharmacokinetics, and toxicity has not been characterized in the available public literature. The compound is available for research purposes only and is not approved for clinical use.
|
| Exact Mass |
243.0808
|
|---|---|
| Elemental Analysis |
C, 64.19; H, 4.14; F, 7.81; N, 17.28; O, 6.58
|
| CAS # |
2328140-37-8
|
| Related CAS # |
139339-45-0; 2328140-37-8; 30195-30-3;
|
| Appearance |
Solid powder
|
| Synonyms |
WUN40378; WUN 40378; WUN-40378; Ro5-3335 analog; Ro 5-3335 analog; Ro 5-3335 analog; Ro 24-7429 analog; Ro 24-7429 analog; Ro24-7429 analog;
|
| 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.) |
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
