WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406465
CAS#: 167467-53-0
Description: BMS-186511 is a Farnesyltransferase (FT) inhibitor with potential anticancer activity. BMS-186511 is a bisubstrate analogue inhibitor of FT, would inhibit the malignant growth properties of a cell line established from malignant schwannoma of an NF1 patient. Following treatment with BMS-186511 , ST88-14 cells became flat, nonrefractile, were contact-inhibited, and lost their ability to grow in soft agar. BMS-186511 was found to specifically inhibit FT, but not geranylgeranyltransferase I, a closely related enzyme. Thus, it is conceivable that FT inhibitors may ultimately become the first generation of drugs against the malignant phenotype in NF1 based on rational insights into the mechanism of action of neurofibromin.
MedKoo Cat#: 406465
Name: BMS-186511
CAS#: 167467-53-0
Chemical Formula: C34H60N3O7PS
Exact Mass: 685.38896
Molecular Weight: 685.89486
Elemental Analysis: C, 59.54; H, 8.82; N, 6.13; O, 16.33; P, 4.52; S, 4.67
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Synonym: BMS186511; BMS 186511; BMS-186511.
IUPAC/Chemical Name: ((5S,8S,11S)-8,11-diisopropyl-5-(methoxycarbonyl)-7,10,13-trioxo-2-thia-6,9,12-triazapentadecan-15-yl)((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)phosphinic acid
InChi Key: QNNCDQUXVSUVDG-QKFLMABSSA-N
InChi Code: InChI=1S/C34H60N3O7PS/c1-23(2)13-11-14-26(7)15-12-16-27(8)17-20-45(42,43)21-18-29(38)36-30(24(3)4)33(40)37-31(25(5)6)32(39)35-28(19-22-46-10)34(41)44-9/h13,15,17,24-25,28,30-31H,11-12,14,16,18-22H2,1-10H3,(H,35,39)(H,36,38)(H,37,40)(H,42,43)/b26-15+,27-17+/t28-,30-,31-/m0/s1
SMILES Code: CSCC[C@@H](C(OC)=O)NC([C@H](C(C)C)NC([C@H](C(C)C)NC(CCP(C/C=C(C)/CC/C=C(C)/CC/C=C(C)\C)(O)=O)=O)=O)=O
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 685.89486 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Yan N, Ricca C, Fletcher J, Glover T, Seizinger BR, Manne V. Farnesyltransferase inhibitors block the neurofibromatosis type I (NF1) malignant phenotype. Cancer Res. 1995 Aug 15;55(16):3569-75. PubMed PMID: 7627966.
2: Carboni JM, Yan N, Cox AD, Bustelo X, Graham SM, Lynch MJ, Weinmann R, Seizinger BR, Der CJ, Barbacid M, et al. Farnesyltransferase inhibitors are inhibitors of Ras but not R-Ras2/TC21, transformation. Oncogene. 1995 May 18;10(10):1905-13. PubMed PMID: 7761092.
3: Manne V, Yan N, Carboni JM, Tuomari AV, Ricca CS, Brown JG, Andahazy ML, Schmidt RJ, Patel D, Zahler R, et al. Bisubstrate inhibitors of farnesyltransferase: a novel class of specific inhibitors of ras transformed cells. Oncogene. 1995 May 4;10(9):1763-79. PubMed PMID: 7753553.
