BMS-214662
Based on 1 Customer Validation
BMS-214662 is a farnesyl transferase inhibitor. BMS-214662 can effectively block the localization and function of Ras protein in the cell membrane by inhibiting the pro-group modification of Ras protein, thereby exerting anti-tumor activity. BMS-214662 has an IC50 value of 1.3 nM for H-Ras and 8.4 nM for K-Ras. BMS-214662 can be used to study Ras-related tumor diseases.
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- Pureté: 99.86%
- CAS No.: 195987-41-8
- Formule: C25H23N5O2S2
- Masse moléculaire:489.61
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)[1]
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | EC50 |
170 nM
Compound: BMS214662
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Inhibition of anchorage-independent growth in human HCT-116 cells assessed as inhibition of colony formation incubated for 14 days in presence of 10% FBS by imaging based soft agar colony formation assay
Inhibition of anchorage-independent growth in human HCT-116 cells assessed as inhibition of colony formation incubated for 14 days in presence of 10% FBS by imaging based soft agar colony formation assay
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[PMID: 16222147] |
| NIH3T3 | EC50 |
0.025 μM
Compound: 20
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Inhibition of anchorage independent growth of H-ras transformed NIH3T3 cells in Soft Agar
Inhibition of anchorage independent growth of H-ras transformed NIH3T3 cells in Soft Agar
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[PMID: 11020273] |
| NIH3T3 | EC50 |
0.025 μM
Compound: 9c, BMS-214662
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Inhibition of FTase in mouse NIH3T3 cells
Inhibition of FTase in mouse NIH3T3 cells
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[PMID: 20925433] |
| NIH3T3 | EC50 |
25 nM
Compound: BMS214662
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Inhibition of anchorage-independent growth in H-Ras transformed mouse NIH3T3 cells assessed as inhibition of colony formation in presence of 10% bovine serum
Inhibition of anchorage-independent growth in H-Ras transformed mouse NIH3T3 cells assessed as inhibition of colony formation in presence of 10% bovine serum
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[PMID: 16222147] |
| NIH3T3 | EC50 |
79 nM
Compound: BMS214662
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Inhibition of anchorage-independent growth in H-Ras transformed mouse NIH3T3 cells assessed as inhibition of colony formation incubated for 14 days in presence of 10% bovine serum by imaging based soft agar colony formation assay
Inhibition of anchorage-independent growth in H-Ras transformed mouse NIH3T3 cells assessed as inhibition of colony formation incubated for 14 days in presence of 10% bovine serum by imaging based soft agar colony formation assay
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[PMID: 16222147] |
BMS-214662 is over 1000-fold selective for farnesyl transferase, having IC50 values for inhibition of geranylgeranylation of Ras-CVLL and K-Ras of 1.3 and 2.3 μM, respectively[1]. BMS-214662 shows good potency in inhibiting H-ras-transformed rodent cells, A2780 human ovarian carcinoma tumor cells, and HCT-116 human colon carcinoma tumor cells. BMS-214662 is the most potent apoptotic FTI known and demonstrates broad spectrum yet robust cell-selective cytotoxic activity against a panel of cell lines with diverse histology[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 195987-41-8
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Appearance Solid
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Masse moléculaire 489.61
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Formule C25H23N5O2S2
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Color White to off-white
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SMILES
N#CC1=CC=C(N(CC2=CN=CN2)C[C@@H](CC3=CC=CC=C3)N(S(=O)(C4=CC=CS4)=O)C5)C5=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : ≥ 100 mg/mL (204.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
The hydrochloride salt of BMS-214662 is dissolved in DMSO with dilutions made using either water or RPMI 1640 plus 10% fetal bovine serum. BMS-214662 is added at various concentrations. The cells are incubated at 37°C for 72 h, at which time MTS in combination with phenazine methosulfate is added. After an additional 3 h, the absorbance is measured at 492 nm, and the growth inhibition results are eventually expressed as IC50s[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: BMS-214662 is dissolved in ethanol, followed by dilution with water to a final ethanol concentration of 10%. Mice implanted with HCT-116 xenografts are administered a single dose of BMS-214662 at 250 mg/kg i.v., 300 mg/kg i.p., or 400 mg/kg p.o. An additional group receives 400 mg/kg BMS-214662 daily for 2 days (administered p.o. on day 1 and i.p. on day 2). Nontreated mice with time-matched HCT-116 tumors served as controls. Tumors are collected at 24 h after dose, processed following standard methods, sectioned, and stained with H&E. Serial sections of each tumor are processed for in situ apoptotic cell labeling by the TUNEL method[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Hunt JT, et al. Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity. J Med Chem. 2000 Oct 5;43(20):3587-95. [Content Brief]
[2]. Rose WC, et al. Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res. 2001 Oct 15;61(20):7507-17. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0424 mL | 10.2122 mL | 20.4244 mL | 51.0611 mL |
| 5 mM | 0.4085 mL | 2.0424 mL | 4.0849 mL | 10.2122 mL | |
| 10 mM | 0.2042 mL | 1.0212 mL | 2.0424 mL | 5.1061 mL | |
| 15 mM | 0.1362 mL | 0.6808 mL | 1.3616 mL | 3.4041 mL | |
| 20 mM | 0.1021 mL | 0.5106 mL | 1.0212 mL | 2.5531 mL | |
| 25 mM | 0.0817 mL | 0.4085 mL | 0.8170 mL | 2.0424 mL | |
| 30 mM | 0.0681 mL | 0.3404 mL | 0.6808 mL | 1.7020 mL | |
| 40 mM | 0.0511 mL | 0.2553 mL | 0.5106 mL | 1.2765 mL | |
| 50 mM | 0.0408 mL | 0.2042 mL | 0.4085 mL | 1.0212 mL | |
| 60 mM | 0.0340 mL | 0.1702 mL | 0.3404 mL | 0.8510 mL | |
| 80 mM | 0.0255 mL | 0.1277 mL | 0.2553 mL | 0.6383 mL | |
| 100 mM | 0.0204 mL | 0.1021 mL | 0.2042 mL | 0.5106 mL |
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