BiochemProbe — Life Science Research Reagents

Lonafarnib free base · Synonyms: SCH66336

Lonafarnib is an orally bioavailable FPTase inhibitor.

For research use only. Not for human or veterinary use.

Purity >98% Stock Inquire

Lonafarnib structure

CAS No.: 193275-84-2

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
250 mg USD 750.00 BP-02337-250mg In stock Get quote
500 mg USD 1,350.00 BP-02337-500mg In stock Get quote
1 g USD 2,150.00 BP-02337-1g In stock Get quote
2 g Inquire BP-02337-2g In stock Inquire
5 g Inquire BP-02337-5g In stock Inquire

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Description

Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively.

Biological activity

Lonafarnib (SCH 66336) is a selectively farnesyl protein transferase (FPT) inhibitor, inhibiting H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib (8 μM) suppresses PKB/Akt activity as well as the phosphorylation of the Akt substrates glycogen synthase kinase (GSK)-3β, forkhead transcription factor, and BAD in SqCC/Y1 cells. Lonafarnib induces a CCAAT/enhancer-binding protein homologous protein (CHOP)-dependent transactivation of the DR5 promoter, thus induces CHOP-dependent DR5 up-regulation.

Identifiers

SMILES
NC(=O)N1CCC(CC(=O)N2CCC(CC2)[C@H]2C3=C(CCC4=C2C(Br)=CC(Cl)=C4)C=C(Br)C=N3)CC1
InChIKey
DHMTURDWPRKSOA-RUZDIDTESA-N

Specifications

MW (average)
638.8220
Formula
C27H31Br2ClN4O2
CAS No.
193275-84-2
Physical state
Solid
Color
White to off-white
Shipping
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
Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

References

1] Liu M, et al. Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. Cancer Res, 1998, 58(21), 4947-4956. [2] Chun KH, et al. Implication of protein kinase B/Akt and Bcl-2/Bcl-XL suppression by the farnesyl transferase inhibitor SCH66336 in apoptosis induction in squamous carcinoma cells. Cancer Res, 2003, 63(16), 4796-4800. [3] Feldkamp MM, et al. Isotype-specific Ras.GTP-levels predict the efficacy of farnesyl transferase inhibitors against human astrocytomas regardless of Ras mutational status. Cancer Res, 2001, 61(11), 4425-4431.