1. Metabolic Enzyme/Protease
  2. Farnesyl Transferase
  3. BMS-214662

BMS-214662 

Cat. No.: HY-16111 Purity: 99.69%
Handling Instructions

BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.

For research use only. We do not sell to patients.

BMS-214662 Chemical Structure

BMS-214662 Chemical Structure

CAS No. : 195987-41-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 452 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 720 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2340 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4080 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.

IC50 & Target

IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)[1]

In Vitro

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].

In Vivo

Tumors from BMS-214662-treated mice have increased numbers of apoptotic cells as compared with the nontreated control mice. The AIs in HCT-116 tumors are increased 4-10-fold in BMS-214662-treated mice as compared with nontreated controls. BMS-214662 is significantly cytotoxic to both HCT-116 and EJ-1 tumor cells; the doses of BMS-214662 required to kill 90% of clonogenic tumor cells are approximately 75 and 100 mg/kg for HCT-116 and EJ-1 tumors[2].

Clinical Trial
Molecular Weight

489.61

Formula

C₂₅H₂₃N₅O₂S₂

CAS No.

195987-41-8

SMILES

N#CC1=CC=C(N(CC2=CN=CN2)C[[email protected]@H](CC3=CC=CC=C3)N(S(=O)(C4=CC=CS4)=O)C5)C5=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (204.24 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0424 mL 10.2122 mL 20.4244 mL
5 mM 0.4085 mL 2.0424 mL 4.0849 mL
10 mM 0.2042 mL 1.0212 mL 2.0424 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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BMS-214662
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