Cdk4/6 Inhibitor IV (Synonyms: CINK4) |
Catalog No.GC11564
One-Click Copy Product Info
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GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 359886-84-3
Sample solution is provided at 25 µL, 10mM.
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Cdk4/6 inhibitor IV is a cell-permeable triaminopyrimidine inhibitor for Cdk4/cyclin D1 and Cdk6/cyclin D1 [1].
Cyclin-dependent kinase 4 (Cdk4) is an important cell cycle kinase, since its activity is required for initiating the phosphorylation of the retinoblastoma protein (pRb). Hyperphosphorylation of pRb prevents cells from initiating DNA synthesis, releases the sequestered transcription factors, leading to the loss of pRb's growth-inhibitory function, thus allowing cells to enter S phase [1].
In vitro: Cdk4/6 inhibitor IV showed an inhibitory effect on Cdk4/cyclin D1 and Cdk6/cyclin D1with the IC50 values of 1.5 and 5.6 μM, respectively. Cdk4/6 inhibitor IV exihibited potent selectivity for Cdk4/6 over Cdk5/p35, c-met, v-abl, IGF-1R, insulin receptor, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D2, Cdk6/cyclin D2, and Cdk1/cyclin B with the IC50 values ≥ 10-100 μM. In asynchronous cell lines, at 5-10 μM, Cdk4/6 inhibitor IV blocked retinoblastoma protein phosphorylation at Ser780 and Ser795, inducing cell cycle arrest in the G1 phase and apoptosis.
In vivo: In mice xenografted with human HCT116 colon carcinoma, treatment with of Cdk4/6 inhibitor IV (i.p, 30 mg/kg) after 29 days suppressed tumor growth.
Reference:
[1] Soni R, O'Reilly T, Furet P, et al. Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4[J]. Journal of the National Cancer Institute, 2001, 93(6): 436-446.
| Cas No. | 359886-84-3 | SDF | |
| Synonyms | CINK4 | ||
| Chemical Name | trans-4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-1H-indol-5-yl]amino]-4-pyrimidinyl]amino]-cyclohexanol | ||
| Canonical SMILES | CCNC1=NC(NC2=CC=C(N(CC3=CC=CC=C3)C=C4)C4=C2)=NC(N[C@H]5CC[C@H](O)CC5)=C1 | ||
| Formula | C27H32N6O | M.Wt | 456.6 |
| Solubility | ≤1mg/ml in ethanol;30mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1901 mL | 10.9505 mL | 21.901 mL |
| 5 mM | 438 μL | 2.1901 mL | 4.3802 mL |
| 10 mM | 219 μL | 1.0951 mL | 2.1901 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)