| Size | Price | Stock | Qty |
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| ln Vitro |
RP-1664 (1-1000 nM, 48-72 h) dose-dependently increases total PLK4 protein levels in RPE1-hTERT Cas9 TP53-deficient cells and increases p21 protein levels in RPE1-hTERT Cas9 TP53 wild-type cells [1]. The sensitivity of RP-1664 (0.001-10 μM) differs by about 30-fold between TRIM37 normal/TP53 knockout cells and TRIM37 overexpression/TP53 wild-type cells, while showing intermediate sensitivity in TRIM37 high expression/TP53 knockout cells and TRIM37 normal/TP53 wild-type cells [1]. RP-1664 (50-250 nM) at concentrations >100 nM induced centrosome loss in both p53-functional and p53-deficient RPE1 cells, as well as in three different NBL cell lines (CHP134, CHP212, and SHSY5Y)[1]. RP-1664 (50-250 nM) at concentrations of 25-100 nM induced the appearance of additional centrosomes in both p53-functional and p53-deficient RPE1 cells[1]. RP-1664 (0-2000 nM, 48 h) enhanced the sensitivity of cells to PLK4 inhibition and centrosome depletion, and this effect depended on high levels of TRIM37 protein and functional p53[1]. RP-1664 (compound 37) reduced the EC50 of MCF7 cell viability by 0.051 μM[2].
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| ln Vivo |
RP-1664 (600 ppm, administered via gavage, 7 days/7 days off or 14 days/7 days off or once daily for 40 days) showed dose-dependent antitumor activity in the MCF7 xenograft mouse model [1]. RP-1664 (300 ppm, administered via gavage, 17 days/7 days off for 40 days) showed significant antitumor activity in the NBL model through low-dose-induced centrosome expansion [1]. RP-1664 (compound 37) (6-21 mg/kg, administered via gavage, twice daily for 35 days) showed dose-dependent tumor growth inhibition, arrest, and regression in the CAL-148 xenograft mouse model [2]. RP-1664 (300-600 ppm, administered orally via feed, for 3 days/4 days off or 14 days/7 days off or daily for 55 days) inhibited tumor growth in CHP-134 xenograft mice [2].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: RPE1-hTERT Cas9 TP53 Deletion Cells and RPE1-hTERT Cas9 TP53 Wild-type Cells Tested Concentrations: 1-1000 nM Incubation Duration: 48-72 hours Experimental Results: Total PLK4 protein levels were elevated in RPE1-hTERT Cas9 TP53 Deletion Cells. p21 protein levels were elevated in a dose-dependent manner in RPE1-hTERT Cas9 TP53 Wild-type Cells. |
| Animal Protocol |
Animal/Disease Models:Female BALB/c nude mice were given estradiol (2.5 µg/mL) in their drinking water and irradiated with γ-rays (1.2 Gy) one week and 24–72 hours before inoculation with 10 million MCF7 cells [1].
Doses: 600 ppm. Route of Administration: Oral administration, with a 7-day dosing/7-day off regimen, a 14-day dosing/7-day off regimen, or daily administration for 40 days. Experimental Results: At a concentration of 600 ppm, the tumor growth inhibition rate (TGI) reached up to 95%. Animal/Disease Models:10 million parental CHP134 cells, CHP134 TP53-KO cells or CHP134 TRIM37-KO cells were inoculated into the right abdomen of female CB/17 SCID mice [1] Doses: 300 ppm Route of Administration: Oral administration, with a 17-day administration/7-day discontinuation regimen for 40 days Experimental Experimental Results: Regardless of whether TRIM37 or TP53 was inactivated, tumor growth was inhibited. Animal/Disease Models:Xenografting of CAL-148 cells (5-7 weeks) in female SCID-Beige mice (107 cells per mouse) [2] Doses: 6, 11, 21 mg/kg Route of Administration: Gavage for 35 days Experimental Results: Tumor growth was inhibited in the 6 mg/kg dose group. Tumor growth was arrested in the 11 mg/kg dose group. Tumor growth regressed in the 21 mg/kg dose group. PLK4 or p21 protein levels increased within 4 to 11 days. Animal/Disease Models:Female CB-17 SCID mice, subcutaneously transplanted with CHP-134 xenograft tumors (5-7 weeks) (107 cells per mouse) [2] Doses: 300, 600 ppm Route of Administration: Oral administration, with a 3-day dosing/4-day off regimen, or a 14-day dosing/7-day off regimen, or daily dosing for 55 days. Experimental Results: Extended dosing time improved tumor regression efficacy. Intermittent dosing improved tolerability, while continuous dosing at 600 ppm was intolerable after day 46. PLK4 or p21 protein levels increased for 4 to 11 days. |
| References |
| Molecular Formula |
C23H24F2N8O2S
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|---|---|
| Molecular Weight |
514.55
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| CAS # |
2980682-00-4
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| Appearance |
White to off-white solid
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| SMILES |
CC1=CC(NC2=NC(N(C3=C(C=C(C=C3F)S(C)(=O)=O)F)C)=NC(C4=CN(C=N4)C)=C2C5CC5)=NN1
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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) |
DMSO : ~100 mg/mL (~194.34 mM; with sonication)
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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 | 1.9434 mL | 9.7172 mL | 19.4345 mL | |
| 5 mM | 0.3887 mL | 1.9434 mL | 3.8869 mL | |
| 10 mM | 0.1943 mL | 0.9717 mL | 1.9434 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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