| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In vitro, BLU2864 (40 nM and 200 nM; 5 d) suppresses cystogenesis caused by forskolin [1].
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|---|---|
| ln Vivo |
In Pkd1RC/RC mice, BLU2864 (oral gavage; 45 mg/kg; once daily; 5 days) inhibits renal PKA activity [1]. In Pkd1RC/RC mice, BLU2864 (oral gavage; 30 mg/kg; once daily; 5 days) reduces PKA activity and enhances PKD [1]. FLC tumor growth is inhibited in vivo by BLU2864 (oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 days) [2].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: mIMCD3 Cell Tested Concentrations: 40 nM and 200 nM Incubation Duration: 5 days Experimental Results: Forskolin-induced in vitro cyst formation of mIMCD3 cells cultured in Matrigel was inhibited at 40 and 200 nM concentrations, respectively. 72% and 100%, respectively, relative to the control. |
| Animal Protocol |
Animal/Disease Models: Pkd1RC/RC mice [1]
Doses: 45 mg/kg Route of Administration: po (oral gavage); 45 mg/kg; one time/day; 5 days Experimental Results: Kidney basis of BLU2864-treated mice compared with control group and total PKA activity were inhibited by 74% and 87%, respectively, at 3 h, and by 46% and 56%, respectively, at 15 h. Animal/Disease Models: Pkd1RC/RC mice [1] Doses: 30 mg/kg Doses: po (oral gavage); 30 mg/kg; one time/day; 5 days Experimental Results: At 15 weeks, BLU2864-treated mice had higher urine output than Control group. demonstrated lower kidney weight, kidney volume as a percentage of body weight, and cyst index. Compared with the control group, renal basal and total PKA activities were diminished by 69% and 84%, respectively, in BLU2864-treated mice. Animal/Disease Models: FLC PDX tumor-bearing mice [2] Doses: 30 mg/kg and 75 mg/kg Route of Administration: po (oral gavage); 30 mg/kg and 75 mg/kg; one time/day; 34-day Experimental Results: Day 3 At 34 days, tumor growth was inhibited by 48.5% (P=0.003) and 45.3% (P=0.0005), respectively. |
| References |
| Molecular Formula |
C24H19F3N4O2
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|---|---|
| Molecular Weight |
452.428475618362
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| Exact Mass |
452.146
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| CAS # |
2810747-89-6
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| PubChem CID |
164603354
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
715
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=CNC2=NC=CC(=C12)C3=NC=C(C=C3)C(=O)N[C@H]4[C@H](CC5=C4C(=CC(=C5)C(F)F)F)O
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| InChi Key |
VRPOVDLLZCQZEG-RXVVDRJESA-N
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| InChi Code |
InChI=1S/C24H19F3N4O2/c1-11-9-30-23-19(11)15(4-5-28-23)17-3-2-12(10-29-17)24(33)31-21-18(32)8-13-6-14(22(26)27)7-16(25)20(13)21/h2-7,9-10,18,21-22,32H,8H2,1H3,(H,28,30)(H,31,33)/t18-,21-/m0/s1
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| Chemical Name |
N-[(1R,2S)-5-(difluoromethyl)-7-fluoro-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)pyridine-3-carboxamide
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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 | 2.2103 mL | 11.0514 mL | 22.1029 mL | |
| 5 mM | 0.4421 mL | 2.2103 mL | 4.4206 mL | |
| 10 mM | 0.2210 mL | 1.1051 mL | 2.2103 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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