| Size | Price | Stock | Qty |
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| ln Vitro |
PVTX-405 (compound 16a) (0.017 nM-10 μM, 6 hours) exhibits excellent novel substrate selectivity and has minimal effect on reducing the protein levels of IKZF1, IKZF3, GSPT1 and CK1α (Dmax <20% at concentrations up to 10 μM) [1]. PVTX-405 (0.01-10000 nM, 1-6 hours) degrades IKZF2 in a CRBN-dependent manner (DC50: 6.3 nM, Dmax: 65%), reaching maximum degradation rate in Jurkat cells within 3 hours [1]. PVTX-405 (1-1000 nM, 24 hours) effectively regulates known IKZF2 transcriptional targets, increases the expression of the inflammatory cytokine IL-2, and reduces the inhibitory activity of Treg cells, thereby promoting the proliferation of effector T cells in Jurkat T cells [1]. PVTX-405 (0.1-1000 nM, 3-6 hours) degrades IKZF2 in a dose-dependent manner, disrupts the stability of human Treg cells, and induces the proliferation of effector T cells[1].
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| ln Vivo |
PVTX-405 (compound 16a) (30 mg/kg, orally, once daily for 21 days) significantly inhibited the growth of MC38 tumors when used alone, and improved the survival rate of animals in combination with anti-PD1 or anti-LAG3 antibodies in MC38 mouse tumor xenograft models (using CrbnI391V C57BL/6 mice)[1].
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| Animal Protocol |
Animal/Disease Models:MC38 cells (5 × 10⁶/mouse) were subcutaneously implanted into Crebn391V C57BL/6 mice [1].
Doses: 30 mg/kg Route of Administration: Oral administration (po) once daily for 21 days, followed by measurement of tumor size and animal weight¹. Experimental Results: Significantly inhibited MC38 tumor growth, with a tumor growth inhibition rate of 68% at the end of treatment. No weight loss or other toxicities were observed during administration to CrebnI391V mice. Significantly delayed the time required for tumors to reach 2000 mm³, improved animal survival, and showed more complete efficacy when used in combination compared to the use of anti-PD-1 or anti-LAG-3 antibodies alone. |
| References |
| Molecular Formula |
C30H31N5O4
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|---|---|
| Molecular Weight |
525.60
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| CAS # |
2991021-08-8
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C1C2=CC=C(C(OC3)=C2CN1[C@@H]4C(NC(CC4)=O)=O)C3(CC5)CCN5CC6=CC(C7=CN(N=C7)C)=CC=C6
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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 | 1.9026 mL | 9.5129 mL | 19.0259 mL | |
| 5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL | |
| 10 mM | 0.1903 mL | 0.9513 mL | 1.9026 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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