| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
CDK7 ≤50 nM (Ki) CDK2 ≥1000 nM (Ki)
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|---|---|
| ln Vitro |
On CDK2 (Ki≥1000 nM) or PLK1 (Ki≥5000 nM), IV-361 exhibits reduced inhibition[1]. Excellent IL-2 and IL-17 production inhibitory activity (all IC50≤100 nM) is demonstrated by IV-361 in peripheral blood mononuclear cells (PBMC)[1]. Excellent HCT-116 cell growth inhibitory action is demonstrated by IV-361 (GI50≤100 nM)[1].
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| ln Vivo |
Orally administered IV-361 (25 mg/kg/day) suppresses tumor volume in female BALB nude mice with HCT-116 at a rate of at least 46%[1].
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| References |
[1]. Noriaki Iwase, et al. Substituted dihydropyrrolopyrazole derivative. US20190256531A1.
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| Molecular Formula |
C23H32FN5O2SI
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|---|---|
| Molecular Weight |
457.62
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| Exact Mass |
457.23
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| CAS # |
2055741-39-2
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| PubChem CID |
140882977
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| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
753
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FYIUNJAFLWNBAI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H32FN5O2Si/c1-14-8-9-15(24)12-17(14)25-21(31)29-13-16-18(22(29,2)3)27-28-19(16)26-20(30)23(10-7-11-23)32(4,5)6/h8-9,12H,7,10-11,13H2,1-6H3,(H,25,31)(H2,26,27,28,30)
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| Chemical Name |
N-(5-fluoro-2-methylphenyl)-6,6-dimethyl-3-[(1-trimethylsilylcyclobutanecarbonyl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-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)
|
| Solubility (In Vitro) |
DMSO : 90 mg/mL (196.67 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (4.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.25 mg/mL (4.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1852 mL | 10.9261 mL | 21.8522 mL | |
| 5 mM | 0.4370 mL | 2.1852 mL | 4.3704 mL | |
| 10 mM | 0.2185 mL | 1.0926 mL | 2.1852 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.
Products are for research use only; We do not sell to patients
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