A potent FTase inhibitor
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BMS 214662

Item No. 28713

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3R)-2,3,4,5-tetrahydro-1-(1H-imidazol-5-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile
CAS Number
195987-41-8
Molecular Formula
C25H23N5O2S2
Formula Weight
489.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: slightly solubleMethanol: slightly soluble
SMILES
O=S(N1CC2=CC(C#N)=CC=C2N(CC3=CN=CN3)C[C@H]1CC4=CC=CC=C4)(C5=CC=CS5)=O
InChi Code
InChI=1S/C25H23N5O2S2/c26-13-20-8-9-24-21(11-20)15-30(34(31,32)25-7-4-10-33-25)23(12-19-5-2-1-3-6-19)17-29(24)16-22-14-27-18-28-22/h1-11,14,18,23H,12,15-17H2,(H,27,28)/t23-/m1/s1
InChi Key
OLCWFLWEHWLBTO-HSZRJFAPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $436

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    Product Description

    BMS 214662 is a potent inhibitor of farnesyltransferase (FTase; IC50 = 1.3 nM).1 It is selective for FTase over geranylgeranyl transferase (GGTase; IC50 = 1,900 nM). It inhibits the growth of MEK2, A2780, and PC3 cancer cells expressing wild-type Ras (IC50s = 2.5, 0.04, and 0.15 μM, respectively), as well as HCT116, MIP, RC-165, and MIA PaCa-2 cells expressing mutant K-Ras (IC50s = 0.06, 0.3, 0.3, and 0.12 μM, respectively). BMS 214662 induces apoptosis in HCT116 cells in a concentration-dependent manner. In vivo, BMS 214662 (600 mg/kg) is curative in an HCT116 mouse xenograft model. It also reduces tumor growth in Calu-1, HT-29, EJ-1, and MIA PaCa-2 mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rose, W.C., Lee, F.Y., Fairchild, C.R., et al. Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res. 61(20), 7507-7517 (2001).