| ln Vitro |
FC-14369 can directly bind to recombinant HIV-1 Nef (NL4-3 variant) with high affinity (Kd = 6.5 nM) and bind to the thalidomide binding domain of CRBN with nanomolar affinity, forming a stable interaction with these two proteins in vitro [1]. FC-14369 (3 μM; 24 h/48 h) can significantly degrade Nef-eGFP in CEM/Nef-eGFP T cells. After 24 hours, the expression of CD4 and MHC-I on the cell surface is restored by about 70%, and after 48 hours, the Nef protein level is reduced to less than 5% of that in the control group [1]. FC-14369 (48 h) can induce Nef degradation in CEM/Nef-eGFP T cells. After 48 hours, the DC50 is 160 nM, and at the active concentration (CC50 = 3.0 μM), targeted degradation can be achieved without producing cytotoxicity [1]. FC-14369 (48 hours) inhibited HIV-1 infection in TZM-bl reporter cells with an IC50 of 250 nM after 48 hours and did not induce cytotoxicity [1]. FC-14369 (1 μM; 4 days) effectively inhibited Nef-dependent HIV-1 replication enhancement in activated human peripheral blood mononuclear cells (PBMCs) with very low cytotoxicity (cell viability ≥90% compared to the control group) after 4 days [1].
|
|---|---|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: Doxycycline-induced CEM/Nef-eGFP human T cells Tested Concentrations: Multiple concentrations Incubation Duration: 48 hours Experimental Results: Nef degradation was induced, with a DC50 (concentration resulting in 50% Nef degradation) of 160 nM. In parallel cell viability assays, the CC50 (concentration resulting in 50% cytotoxicity) was approximately 3.0 μM. |
| References |
|
| CAS # |
3066894-28-5
|
|---|---|
| Appearance |
Light yellow to green yellow solid
|
| 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 Note: 请将本产品存放在密封且受保护的环境中（例如氮气下），避免暴露在潮湿环境中。 |
| 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) |
DMSO : ~100 mg/mL (~116.93 mM; with sonication)
|
|---|---|
| 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
