| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
In the G2/M phase, PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) stimulates cell cycle cycling [1]. The DETAC CDK2/9 Degrader-1 (500 nM; 2-24) effectively degrades CDK2/9 in cells with strong CDK2/9 expression, including MCF-7, HCT-116, and 22Rv1 [1]. It also initializes PC-3. CDK2 and CDK9 are inhibited by /9 Degrader-1, with IC50 values of 7.42 nM and 14.50 nM, respectively [1].
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|---|---|
| Cell Assay |
Cell cycle analysis [1]
Cell Types: PC-3 Cell Tested Concentrations: 500 nM Incubation Duration: 2, 4, 8, 16, 24 hrs (hours) Experimental Results: Mcl-1 protein levels were down-regulated in PC-3 cells. Western Blot Analysis[1] Cell Types: PC-3 Cell Tested Concentrations: 0.25, 1, 3 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced cell cycle arrest in G2/M phase. |
| References |
| Molecular Formula |
C₄₀H₄₁N₁₃O₇
|
|---|---|
| Molecular Weight |
815.84
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| Exact Mass |
815.325
|
| CAS # |
2408641-24-5
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| PubChem CID |
145925673
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| Appearance |
White to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.749
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| LogP |
0.75
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
60
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| Complexity |
1620
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BRYMZSSAIDEFEM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C40H41N13O7/c54-30(42-15-14-41-27-3-1-2-25-33(27)40(60)53(39(25)59)29-8-9-31(55)49-37(29)57)10-11-32(56)52-18-16-51(17-19-52)21-23-4-6-24(7-5-23)47-38(58)34-28(20-46-50-34)48-36-26-12-13-43-35(26)44-22-45-36/h1-7,12-13,20,22,29,41H,8-11,14-19,21H2,(H,42,54)(H,46,50)(H,47,58)(H,49,55,57)(H2,43,44,45,48)
|
| Chemical Name |
N-[4-[[4-[4-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethylamino]-4-oxobutanoyl]piperazin-1-yl]methyl]phenyl]-4-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamide
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| Synonyms |
PROTAC CDK2/9 Degrader1; PROTAC CDK2/9 Degrader 1
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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 : ~55 mg/mL (~67.42 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (6.13 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2257 mL | 6.1287 mL | 12.2573 mL | |
| 5 mM | 0.2451 mL | 1.2257 mL | 2.4515 mL | |
| 10 mM | 0.1226 mL | 0.6129 mL | 1.2257 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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