BMS-214662 hydrochloride

Cat. No.: HY-16111A Purity: 98.54%: Data Sheet
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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.

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

BMS-214662 hydrochloride Chemical Structure

CAS No. : 195981-08-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Other Forms of BMS-214662 hydrochloride:

BMS-214662 In-stock

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K-Ras H-Ras N-Ras Ras

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

In Vitro

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.

In Vivo

Compared to untreated control mice, the number of apoptotic cells in tumors from mice treated with BMS-214662 increased. The Apoptotic Index (AI) in HCT-116 tumors from BMS-214662-treated mice increased by 4-10 times compared to the untreated control group. BMS-214662 exhibited significant cytotoxicity against HCT-116 and EJ-1 tumor cells; the doses of BMS-214662 required to kill 90% of clonogenic tumor cells were approximately 75 and 100 mg/kg for HCT-116 and EJ-1 tumors, respectively^[2].

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

Molecular Weight

526.07

Formula

C₂₅H₂₄ClN₅O₂S₂

CAS No.

195981-08-9

Appearance

Solid

Color

Off-white to light brown

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9009 mL	9.5044 mL	19.0089 mL
5 mM	0.3802 mL	1.9009 mL	3.8018 mL
10 mM	0.1901 mL	0.9504 mL	1.9009 mL

View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.54%

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Data Sheet (282 KB) SDS (393 KB)

COA (261 KB) HNMR (486 KB) RP-HPLC (155 KB) LCMS (98 KB)

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

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