G2035-20
Imatinib, Methanesulfonate Salt (STI-571, CGP-57148B)
Größe
£152.00
- SKU:
- G2035-20
- Molekulargewicht:
- 589.71
- Reinheit:
- HPLC: ≥98%, TLC: ≥98%
- Lagerbedingungen:
- -20°C
- Hersteller:
- United States Biological
- CAS Number:
- 220127-57-1
- Format:
- Supplied as a off-white to white powder
- Weitere Details:
- A tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Imatinib inhibits bcr-abl tyrosine kinase activity, upon which some types of tumor cells depend for growth. Imatinib acts by binding to the ATP binding site of bcr-abl and competitively inhibiting its tyrosine kinase activity. Imatinib is selective for bcr-abl, but it also targets several other kinases (c-kit and PDGF-R). (1) Imatinib also stimulates the entry of the bcr-abl tyrosine kinase into the nucleus, where it cannot perform its anti-apoptopic functions. (2) Imatinib inhibits EOL-1 cell viability (IC50 = 0.5 nM), phosphorylation of a fusion protein (IC50 = 30 nM), and viability of BaF3 cells expressing Rhe-PDGFRα in the absence of IL-3 (IC50 = 0.17 nM). (3) Inhibition of CSF-1R by imatinib is competitive with ATP, with a Ki value of 120nM. (4) The IC50 values for imatinib inhibition of KBM5 and KBM7 cell growth were about 0.48 and 0.24 µM, respectively, while the IC50 values for imatinib in KBM5-STI571R1.0 and KBM7-STI571R1.0 cells were about 6.40 and 3.30uM, respectively. (The data were from figure 2 but we found several errors in the figure. The correct data cannot be determined without further information). The calculated resistance indexes for imatinib were 13.3 for KBM5-STI571R1.0 cells and 13.8 for KBM7-STI571R1.0 cells. (5) Imatinib is the active ingredient in the drug sold under the trade name Gleevec® in USA or Glivec in Europe and Australia. This drug has been approved in at least one country for use in patients with gastrointestinal stromal tumors, chronic myelogenous leukemia and a number of other malignancies. NOTE: The imatinib sold by LC Laboratories is NOT Gleevec® or Glivec, and is NOT for human use. Solubility: Soluble in DMSO at 100mg/ml. Very poorly soluble in ethanol; soluble in water at 200mg/ml.; buffers, serum or other additives may increase or decrease the aqueous solubility. Elemental Analysis: Calculated: C: 61.10% H: 5.98% N: 16.63% S: 5.44% Storage and Stability: May be stored at RT for short-term only. Long-term storage is recommended at -20°C for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
- Versandbedingungen:
- Ambient