| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| Targets |
Cdk4/cyclin D1 (IC50 = 1.5 μM); CDK6/cyclinD1 (IC50 = 5.6 μM); CDK5/p35 (IC50 = 25 μM); CDK2/cyclinA (IC50 >50 μM); CDK1/cyclinB (IC50 >100 μM); CDK2/cyclin E (IC50 >50 μM); CDK4/cyclin D2 (IC50 >50 μM); Cdk6/cyclin D2 (IC50 >50 μM); V-abl (IC50 >10 μM); c-met (IC50 >10 μM); IGF-1R (IC50 >10 μM); Insulin-R (IC50 >10 μM)
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|---|---|
| ln Vitro |
GP-82996 (5, 10 μM; 24 hours) causes an increase in the G0-G1/S ratio and G1 arrest in p16 positive (MRC-5) and p16 negative (U2OS) cells[1].GP-82996 (5, 10 μM; 24 hours) decreases pRb hyperphosphorylation, but does not alter CDK4 levels in MRC-5 and U2OS cells[1].
GP-82996 (5, 10 μM; 48 hours) causes 83% of U2OS cells to undergo apoptosis when exposed to a concentration of 10μM[1].
GP-82996 (0.1–40 μM; 24, 48, and 72 hours) inhibits A549, H358, SKLU-1, H23, and PC14 cells' ability to proliferate; at 72 hours, the IC50 values are 4–7 μM[2].
GP-82996 (3, 5, 10 μM; 48 hours) causes H23 and A549 cells to go into G1 arrest[2].
GP-82996 ((1, 3, 5, 10 μM; 72 hours) increases the sensitivity of Paclitaxel in lung cancer cells (A549, SKLU-1, H23 cells) harboring KRAS mutations [2].
GP-82996 (10 μM; 72 hours) increases the apoptosis of A549 and H23 cells when combined with Paclitaxel (3 nM; 72 hours)[2].
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| ln Vivo |
GP-82996 (30 mg/kg, intraperitoneal for 29 days) in mouse xenograft models results in a reduced final tumor volume when compared to vehicle control[1].
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| Animal Protocol |
19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)[1]
30 mg/kg i.p. every 12 hours for 29 days |
| References |
|
| Molecular Formula |
C27H32N6O
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|---|---|
| Molecular Weight |
456.58
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| Exact Mass |
456.26375967
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| CAS # |
359886-84-3
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| Related CAS # |
359886-84-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
CCNC1=CC(=NC(=N1)NC2=CC3=C(C=C2)N(C=C3)CC4=CC=CC=C4)NC5CCC(CC5)O
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| InChi Key |
YVXCDLCJCIDFHE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H32N6O/c1-2-28-25-17-26(29-21-8-11-23(34)12-9-21)32-27(31-25)30-22-10-13-24-20(16-22)14-15-33(24)18-19-6-4-3-5-7-19/h3-7,10,13-17,21,23,34H,2,8-9,11-12,18H2,1H3,(H3,28,29,30,31,32)
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| Chemical Name |
4-[[2-[(1-benzylindol-5-yl)amino]-6-(ethylamino)pyrimidin-4-yl]amino]cyclohexan-1-ol
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| Synonyms |
CINK-4; GP-82996
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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 | 2.1902 mL | 10.9510 mL | 21.9020 mL | |
| 5 mM | 0.4380 mL | 2.1902 mL | 4.3804 mL | |
| 10 mM | 0.2190 mL | 1.0951 mL | 2.1902 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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