Bms-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50 of 100 nM and 73 nM, respectively. It also showed moderate inhibitory activity against Mek, Fak and Lck, but almost no inhibitory activity against Akt1 and MAPK1/2.
 |
Source | Onco Targets Ther (2015). Figure 1. BMS-536924 |
| Method | cell viability assay | |
| Cell Lines | TMZ-resistant cells | |
| Concentrations | 400 nM | |
| Incubation Time | 24, 48, or 72 h | |
| Results | BMS-536924 also significantly reduced the viability of both TMZ-sensitive and -resistant lines, in a time-dependent manner |
| Cell Experiment | |
|---|---|
| Cell lines | TGBC-1TKB, TGBC-2TKB and TGBC-14TKB cell lines |
| Preparation method | In vitro cell growth. Four thousand cells were seeded into a 96-well plate and each was treated with several concentrations of BMS-536924. Cell growth was measured using WST-1 reagent (Roche, Basel, Switzerland), as described previously. |
| Concentrations | 0, 1, 5, 10μM |
| Incubation time | 0, 1, 2, 3, 4 days |
| Animal Experiment | |
|---|---|
| Animal models | TGBC-1TKB tumour xenograft in nude mice |
| Formulation | a mixture of polyethylene glycol 400 (PEG400 ⁄ water, 4:1 vol ⁄ vol) |
| Dosages | 70 mg ⁄ kg once daily for 2 weeks |
| Administration | oral gavage |
| Molecular Weight | 479.96 |
| Formula | C25H26ClN5O3 |
| CAS Number | 468740-43-4 |
| Solubility (25°C) | DMSO 66 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related IGF-1R Products |
|---|
| IGF-I (24-41)
IGF-I (24-41) (Insulin-like Growth Factor I (24-41)) is amino acids 24 to 41 fragment of IGF-I. |
| GIP, human
GIP, human is a peptide hormone consisting of 42 amino acids that also acts as a promoter of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. In addition, GIP, human acts as an enteric proinsulin hormone released by intestinal K cells in response to nutrient intake. |
| VMB-100
VMB-100 is an engineered mRNA molecule encoding human insulin-like growth factor-1 (IGF-1) that induces IGF-1 expression in human muscle cells. |
| NBI-31772 hydrate
NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (Kis=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects. |
| AZ12253801
AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
