BMS-214662 hydrochloride
Based on 1 Customer Validation
BMS-214662 hydrochloride is an inhibitor of farnesyltransferase (Farnesyl Transferase). BMS-214662 hydrochloride can effectively block the localization and function of Ras proteins on the cell membrane by inhibiting the prenylation modification of Ras proteins, thereby exerting anti-tumor activity. The IC50 value of BMS-214662 hydrochloride for H-Ras is 1.3 nM, and for K-Ras it is 8.4 nM. BMS-214662 hydrochloride can be used in the research of tumor diseases related to Ras.
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- Purity: 98.54%
- CAS No.: 195981-08-9
- 화학식: C25H24ClN5O2S2
- 분자량:526.07
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보관:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)[1]
BMS-214662 has over 1000 times selectivity for farnesyltransferase, with IC50 values for inhibiting geranylgeranylation of Ras-CVLL and K-Ras at 1.3 and 2.3 μM, respectively[1]. BMS-214662 demonstrates 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 effective apoptotic FTI known and exhibits broad-spectrum but 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.
Chemical Information
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CAS No. 195981-08-9
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Appearance Solid
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분자량 526.07
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화학식 C25H24ClN5O2S2
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Color Off-white to light brown
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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.Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
용액&용해도
DMSO : ≥ 100 mg/mL (190.09 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9009 mL | 9.5044 mL | 19.0089 mL | 47.5222 mL |
| 5 mM | 0.3802 mL | 1.9009 mL | 3.8018 mL | 9.5044 mL | |
| 10 mM | 0.1901 mL | 0.9504 mL | 1.9009 mL | 4.7522 mL | |
| 15 mM | 0.1267 mL | 0.6336 mL | 1.2673 mL | 3.1681 mL | |
| 20 mM | 0.0950 mL | 0.4752 mL | 0.9504 mL | 2.3761 mL | |
| 25 mM | 0.0760 mL | 0.3802 mL | 0.7604 mL | 1.9009 mL | |
| 30 mM | 0.0634 mL | 0.3168 mL | 0.6336 mL | 1.5841 mL | |
| 40 mM | 0.0475 mL | 0.2376 mL | 0.4752 mL | 1.1881 mL | |
| 50 mM | 0.0380 mL | 0.1901 mL | 0.3802 mL | 0.9504 mL | |
| 60 mM | 0.0317 mL | 0.1584 mL | 0.3168 mL | 0.7920 mL | |
| 80 mM | 0.0238 mL | 0.1188 mL | 0.2376 mL | 0.5940 mL | |
| 100 mM | 0.0190 mL | 0.0950 mL | 0.1901 mL | 0.4752 mL |
BMS-214662 hydrochloride Related Classifications
HY-16111A Related Classifications
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