S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies.
| Molecular Weight | 502.49 |
| Formula | C27H21F3N6O |
| CAS Number | 1257628-57-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 32 mg/mL (ultrasonic and warming and heat to 60°C) |
| Storage | 4°C, sealed |
| 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.
