Tipifarnib CAS No.: 192185-72-1

Tipifarnib CAS No.: 192185-72-1 – A Comprehensive Guide

Tipifarnib, also known as Zarnestra, is a potent and selective farnesyltransferase inhibitor. Farnesyltransferase plays a crucial role in cancer cell proliferation and is a promising target for cancer therapy. Tipifarnib is well-known for its potential to inhibit the proliferation of various types of cancer cells, including leukemia, breast cancer, melanoma, and pancreatic cancer. As a manufacturer of this innovative drug, we take pride in introducing this life-changing product to merchants worldwide, helping them make a difference in the world of medicine.

Composition and Properties

Tipifarnib is a synthetic tetrahydroquinoline compound that selectively inhibits farnesyltransferase, thereby preventing the activation of oncogenic Ras proteins. The compound has a molecular formula of C27H28ClN5O2, with a molecular weight of 491. Performed primarily as a white to off-white powder or crystalline solid, Tipifarnib is soluble in ethanol, dimethyl sulfoxide (DMSO), and methanol.

Mechanism of Action

Tipifarnib works by inhibiting the farnesyltransferase enzyme, which adds a farnesyl group to specific signaling proteins, including members of the Ras family, at their C-terminus. This farnesylation is necessary for the membrane attachment of these proteins and is critical to cell signaling, proliferation, and differentiation. Inhibition of farnesyltransferase by Tipifarnib leads to the accumulation of unfarnesylated Ras proteins in the cytosol, depriving them of their signaling function, resulting in cancer cell death.

Applications

Tipifarnib is a highly selective inhibitor of farnesyltransferase, which makes it more effective in cancer treatment than other Ras inhibitors. It has shown potential in multiple cancer types, mainly hematologic malignancies, specifically acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). Tipifarnib is the only drug that has demonstrated clinical activity in the treatment of advanced or refractory AML with an HRAS mutation. It is also highly effective in targeting other Ras mutations and gene fusions, specifically KRAS, NRAS, HRAS, and BRAF. Therefore, Tipifarnib is a vital medication in the development of cancer therapies that target Ras-mutated cancers.

Advantages

Tipifarnib has several advantages over other chemotherapeutic agents, including:

1. A highly selective inhibitor of farnesyltransferase, which makes it highly efficient in cancer treatment.

2. It has a minimal affinity for cytochrome P450 enzymes, and thus it exhibits low drug interaction.

3. It has an excellent pharmacokinetic profile characterized by a high oral bioavailability, a long half-life, and slow clearance, allowing for less frequent dosing.

4. It has shown a favorable safety profile, with most side effects being mild to moderate and reversible.

5. It is a promising drug candidate for combination therapy with other anticancer drugs.

Conclusion

Tipifarnib is an innovative and potent farnesyltransferase inhibitor that has shown promise in cancer treatment. It is highly selective, effective, and with a favorable safety profile. As a manufacturer of this crucial medical drugs, we strive to ensure its availability and accessibility to merchants worldwide. We believe that this product will make a significant impact on the world of medicine, not only in cancer treatment but also in the development of therapies that target Ras-mutated cancers. We welcome inquiries from interested merchants and are committed to providing them with high-quality products at competitive prices.

Chemical Structure: Tipifarnib

CAS No.: 192185-72-1

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R115777(IND 58359; Tipifarnib; IND-58359; IND58359; R-115777;R 115777)

Catalog No.: URK-V593 Only Used For Lab.

R11577(Tipifarnib, IND-58359), have potential antineoplastic activity, is a potent and selective inhibitor of FTase (farnesyltransferase) with an IC₅₀ of 0.86 nM,

Biological Activity

Tipifarnib (IND 58359, R115777) is a potent inhibitor of Tryanosoma Cruzi with the ED50 of 4mM[1]; inhibits the farnesylation of lamin B and K-RasB peptide substrates with IC50s of 0.86 nM and 7.9 nM, respectively[2]; no activity for PGGT1(IC50>50 uM); shows sensiticity for tumor cell lines bearing H-ras or N-ras mutations; inhibits the growth of tumors bearing mice and orally bioavailable, inhibits the Steatohepatitis
Phase 2 Clinical

Physicochemical Properties

References

1.Devendra S Puntambekar, et al. Inhibition of farnesyltransferase: a rational approach to treat cancer? J Enzyme Inhib Med Chem. 2007 Apr;22(2):127-40.

2.End DW, et al. Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res. 2001 Jan 1;61(1):131-7

3.Kelland LR, et al. Clin Cancer Res. 2001 Nov;7(11):3544-50.

4.Beaupre DM, et al. Mol Cancer Ther. 2004 Feb;3(2):179-86.

URK-V593_COA

URK-V593_SDS

URK-V593_TDS

 

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