SU6656 is a small-molecule, indolinone which potently and selectively inhibits Src tyrosine kinases, which are known to function in signal transduction pathways.SU6656 can induce polyploidy in cells of lymphoid origin, revealing a chemotherapeutic potential for this inhibitor to limit tumor propagation of malignant B cell lymphomas, although not without affecting normal B cells as well.Clonogenic survival of endothelial cells was decreased after the combined therapy of SU6656 and radiation compared with radiotherapy alone.Furthermore, SFK inhibition by SU6656 attenuated radiation-induced Akt phosphorylation and increased radiation-induced apoptosis and vascular endothelium destruction.In vivo, SU6656 administered before irradiation significantly enhanced radiation-induced destruction of blood vessels within the tumor windows and enhanced tumor growth delay when administered during fractionated irradiation.SU6656 might be useful as a differentiation-inducing agent for MKs and is an important tool for understanding the molecular basis of MK endomitosis. SU6656 should prove a useful additional tool for further dissecting the role of Src kinases in this and other signal transduction pathways.
 |
Source | Blood Adv (2018). Figure 2. SU6656 |
| Method | In vitro culture of CD341 HPCs into megakaryocytes | |
| Cell Lines | CD341 HPCs | |
| Concentrations | 2.5 μM | |
| Incubation Time | 4 days | |
| Results | Each small inhibitor, SU6656, Y27632, and AZD1152, effects distinct intracellular pathways, yet all enhance the degree of polyploidism of the resultant megakaryocytes |
| Molecular Weight | 371.45 |
| Formula | C19H21N3O3S |
| CAS Number | 330161-87-0 |
| Solubility (25°C) | DMSO 50 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 Src-bcr-Abl Products |
|---|
| Asciminib hydrochloride
Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM. |
| Osteogenic Growth Peptide (10-14)
Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. |
| Abl Cytosolic Substrate
Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ). |
| Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). |
| p60c-src substrate II
p60c-src substrate II is an efficient pentapeptide substrate for the tyrosine kinase pp60c-src. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
