| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| ln Vitro |
CDK2 degrader 6 (compound 6) (24 hours) effectively induced the degradation of CDK2 in CDK2 HiBiT-labeled HEK293 cells. After 24 hours of treatment, the CDK2 protein level decreased by a maximum of 62.0%, and the DC50 was 46.5 nM [1]. CDK2 degrader 6 (24 hours) showed very low degradation activity against GSPT1 in GSPT1 HiBiT-labeled HEK293 cells. After 24 hours of treatment, the GSPT1 protein level decreased by a maximum of only 9.9% [1]. CDK2 degrader 6 (0.316-1000 nM; 7 days) effectively inhibited the proliferation of MDA-MB-157 breast cancer cells. After 7 days of treatment, the cell proliferation was inhibited by a maximum of 90%, and the EC50 was 10 nM [1]. CDK2 degrader 6 (152 nM-1000 nM; 24 hours) can effectively induce the degradation of CDK2 protein in MDA-MB-157 breast cancer cells. After 24 hours of treatment, the CDK2 level decreased by up to 84%, and the DC50 was 4 nM [1]. CDK2 degrader 6 (10-1000 nM; 24 hours) can disrupt the cell cycle of MDA-MB-157 breast cancer cells. After 24 hours of treatment at concentrations of 10 nM to 1000 nM, dose-dependent G1 phase arrest and S phase cell reduction can be achieved [1].
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| ln Vivo |
CDK2 degrader 6 (compound 6) (30-100 mg/kg; orally; twice daily; 21 days) showed significant antitumor activity in MKN1 gastric cancer xenografts, with TGI of 45% and 47%, respectively[1].
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| Animal Protocol |
Animal/Disease Models:Mice injected with MKN1[1]
Doses: 30 mg/kg; 100 mg/kg Route of Administration:Oral; twice daily; 21 days Experimental Results:The tumor growth inhibition rate (TGI) reached 45% on day 21, which was statistically significant compared with the vector group. The tumor growth inhibition rate (TGI) reached 47% on day 21, which was statistically significant compared with the vector group. |
| References |
| Molecular Formula |
C23H22F5N5O3
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|---|---|
| Molecular Weight |
511.44
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| CAS # |
3036606-92-2
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| Related CAS # |
(R)-CDK2 degrader 6
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| Appearance |
Off-white to light yellow solid
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| SMILES |
O=C(C(CC1)C2=C(F)C=C(N3C[C@H](NC4=NN=C(C56CC(C6)(C(F)(F)F)C5)O4)[C@H]3C)C=C2F)NC1=O
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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 Note: 请将本产品存放在密封且受保护的环境中（例如氮气下），避免暴露在潮湿环境中。 |
| 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 : ~15 mg/mL (~29.33 mM; with sonication and warming)
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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 | 1.9553 mL | 9.7763 mL | 19.5526 mL | |
| 5 mM | 0.3911 mL | 1.9553 mL | 3.9105 mL | |
| 10 mM | 0.1955 mL | 0.9776 mL | 1.9553 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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