| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
CI-988 has a strong affinity (Ki of 4.5 nM) to block the specific binding of 125I-BH-CCK-8 to NCI-H727 cells. When CCK-8 is added to NCI-727 cells, it causes a rise in ROS, which CI-988 can effectively prevent. NCI-H727 cells or cells activated with CCK-8 exhibit basal growth inhibition from CI-988 (3 µM). The capacity of CCK-8 to phosphorylate ERK and raise cytosolic Ca2+ is inhibited by CI-988. [1]. In a dosage-dependent way, CI-988 prevents CCK-8 from activating EGFR in NCI-H727 cells. The effects of 0.1 µM CCK-8 on EGFR tyrosine phosphorylation were slightly and severely suppressed by CI-988 at 1 µM and 10 µM, respectively. When it comes to EGFR or ERK tyrosine phosphorylation in lung cancer, CI-988 opposes CCK-8's ability to do so [1].
|
|---|---|
| ln Vivo |
In xenograft model mice, CI-988 (10 mg/kg; oral; daily; for 20 days) inhibits the growth of colorectal cancer [3].
|
| Animal Protocol |
Animal/Disease Models: Nude mice were injected with LoVo cells [3]
Doses: 10 mg/kg Route of Administration: po; daily; 20-day Experimental Results: inhibited the growth of xenografts by 53%. |
| References |
|
| Molecular Formula |
C35H42N4O6
|
|---|---|
| Molecular Weight |
614.74
|
| Exact Mass |
614.31
|
| CAS # |
130332-27-3
|
| PubChem CID |
108187
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.32g/cm3
|
| Boiling Point |
949.6ºC at 760mmHg
|
| Vapour Pressure |
0mmHg at 25°C
|
| Index of Refraction |
1.647
|
| LogP |
6.031
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
13
|
| Heavy Atom Count |
45
|
| Complexity |
1070
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC(CC1=CNC2=CC=CC=C21)(C(=O)NCC(C3=CC=CC=C3)NC(=O)CCC(=O)O)NC(=O)OC4C5CC6CC(C5)CC4C6
|
| InChi Key |
FVQSSYMRZKLFDR-ZABPBAJSSA-N
|
| InChi Code |
InChI=1S/C35H42N4O6/c1-35(18-26-19-36-28-10-6-5-9-27(26)28,39-34(44)45-32-24-14-21-13-22(16-24)17-25(32)15-21)33(43)37-20-29(23-7-3-2-4-8-23)38-30(40)11-12-31(41)42/h2-10,19,21-22,24-25,29,32,36H,11-18,20H2,1H3,(H,37,43)(H,38,40)(H,39,44)(H,41,42)/t21?,22?,24?,25?,29-,32?,35+/m0/s1
|
| Chemical Name |
4-[[(1R)-2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
|
| Synonyms |
CI-988 CI988CI 988 PD-134,308PD-134308PD 134308
|
| HS Tariff Code |
2934.99.9001
|
| 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) |
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
|
|---|---|
| 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 | 1.6267 mL | 8.1335 mL | 16.2670 mL | |
| 5 mM | 0.3253 mL | 1.6267 mL | 3.2534 mL | |
| 10 mM | 0.1627 mL | 0.8134 mL | 1.6267 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
