| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
BMS-605541 primarily targets vascular endothelial growth factor receptor-2 (VEGFR-2), a receptor tyrosine kinase that mediates angiogenesis. By inhibiting VEGFR-2 kinase activity, BMS-605541 blocks VEGF signaling, which is essential for endothelial cell proliferation, migration, and survival. It has an IC50 of 23 nM for VEGFR-2. It also inhibits Flk-1 (mouse VEGFR-2), VEGFR-1, and PDGFR-β.
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| ln Vitro |
BMS-605541 (Compound 14) inhibits HUVEC growth via VEGF, with an IC50 value of 25 nM[1].
In vitro, BMS-605541 is a potent inhibitor of VEGFR-2 with an IC50 of 23 nM. It inhibits VEGF-induced proliferation in human umbilical vein endothelial cells (HUVECs) with an IC50 of 25 nM. It is selective for VEGFR2 over 22 other kinases. It also inhibits Flk-1, VEGFR-1, and PDGFR-β with IC50 values of 40 nM, 400 nM, and 200 nM, respectively. |
| ln Vivo |
Anti-tumor effect of BMS-605541 (12.5-180 mg/kg; once or twice daily for 14 days) has been seen against HCT-116 xenografts and athymic electrodes of subcutaneous inlet L2987 [1]. 605541's pharmacokinetic (PK) parameters [1] include species administration, dosage (mg/kg), Cmax (μM), Tmax (h), AUC (μM·h), T1/2 (h), MRT (h), Cl (mL/min·kg), Vss (L/kg), and Fpo (%). Oral gavage in mice is 90 148 0.5 649 (0-24 h) 1.7 3.4 100. Intravenous injection in rats is 50 44.0 2.0 202 2.2 3.5 100 Rat oral gavage is 10 13.6 1.1 100. Cyno oral gavage in rats is 5 8.0 0.75 28.5 7.1 7.9 52. Cyno intravenous injection is 1 3.9 1.6 52.
In vivo, BMS-605541 is an orally active compound that has been studied for its potential in cancer research. By inhibiting VEGFR-2-mediated angiogenesis, it may reduce tumor growth and metastasis. Its selectivity for VEGFR2 over other kinases suggests a favorable safety profile. Further studies are needed to fully characterize its in vivo efficacy and safety in animal models of cancer. |
| Enzyme Assay |
The in vitro activity of BMS-605541 is assessed using cell-free kinase activity assays. Recombinant VEGFR-2 kinase is incubated with a substrate peptide and ATP in the presence of varying concentrations of BMS-605541. The phosphorylation of the substrate is measured, typically using a radioactive (e.g., [γ-³²P]ATP) or fluorescence-based method. The IC50 is determined from dose-response curves.
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| Cell Assay |
For cellular assays, human umbilical vein endothelial cells (HUVECs) are cultured in appropriate media. Cells are treated with various concentrations of BMS-605541 (typically 1-1000 nM) for defined periods. VEGF-induced proliferation is assessed using MTT or CellTiter-Glo assays. The phosphorylation of VEGFR-2 and downstream signaling molecules (e.g., Akt, ERK) is analyzed by Western blotting using phospho-specific antibodies. Cell migration and tube formation assays are performed.
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| Animal Protocol |
In vivo, BMS-605541 is typically administered orally to mice bearing tumor xenografts. The compound is formulated in a suitable vehicle and administered at various doses daily. Tumor growth is monitored by measuring tumor volume. At the end of the study, tumors are excised and analyzed for angiogenesis (CD31 staining), proliferation (Ki-67), and apoptosis (TUNEL). Pharmacokinetic studies involve measuring BMS-605541 levels in plasma.
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| ADME/Pharmacokinetics |
BMS-605541 has a molecular weight of 401.43 g/mol and a molecular formula of C19H17F2N5OS. It is a selective and orally active VEGFR-2 inhibitor. The compound should be stored as a powder at -20°C under desiccated conditions. Specific solubility and pharmacokinetic parameters are not detailed in the provided search results. It is soluble in DMSO and other organic solvents.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BMS-605541 is not available in the provided search results. As a VEGFR-2 inhibitor, it may affect angiogenesis, which is important for wound healing and reproductive function. The compound is intended for research purposes only and is not approved for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies are required to establish its full safety profile.
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| References | |
| Additional Infomation |
BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase. It has an IC50 of 23 nM for VEGFR-2 and inhibits VEGF-induced proliferation in HUVECs. It is selective for VEGFR2 over 22 other kinases. BMS-605541 also inhibits Flk-1, VEGFR-1, and PDGFR-β. It is a valuable tool for studying angiogenesis and for cancer research. The compound is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C19H17F2N5OS
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|---|---|
| Molecular Weight |
401.4358
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| Exact Mass |
401.112
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| CAS # |
639858-32-5
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| PubChem CID |
11632737
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.660
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| LogP |
1.95
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
541
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC1NC(=O)C2=CC(=C(C=C2F)F)NCC3=CN=C(S3)NC4=CC=CC=N4
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| InChi Key |
CUPLTRAPYIXFAX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17F2N5OS/c20-14-8-15(21)16(7-13(14)18(27)25-11-4-5-11)23-9-12-10-24-19(28-12)26-17-3-1-2-6-22-17/h1-3,6-8,10-11,23H,4-5,9H2,(H,25,27)(H,22,24,26)
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| Chemical Name |
N-cyclopropyl-2,4-difluoro-5-[[2-(pyridin-2-ylamino)-1,3-thiazol-5-yl]methylamino]benzamide
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| Synonyms |
BMS605541; BMS 605541; BMS-605541
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~83.03 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4910 mL | 12.4552 mL | 24.9103 mL | |
| 5 mM | 0.4982 mL | 2.4910 mL | 4.9821 mL | |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4910 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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