Free shipping on all orders over $ 500
AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro. AZ32 is highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free-brain concentrations of AZ32 are in excess of the cellular IC50 for approximately 22 hours.
| Cell Experiment | |
|---|---|
| Cell lines | U1242 cells |
| Preparation method | Human glioma U1242 cells were treated with AZ32 (3 μM) and radiation (2 Gy) or left untreated. At 48 hrs the cells were fixed and processed for ICC using anti-γ-tubulin (centrosomes) and -α-tubulin (microtubules). Cells were counterstained with DAPI to visualize nuclei. |
| Concentrations | 3 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | orthotopic GL261 glioma model (GL261/luc-red cells intracranially injected into C57bl6 mice) |
| Formulation | in hydroxypropyl-methyl cellulose (0.5%w/v)/0.1%w/v polysorbate-80 to 20 mg/ml |
| Dosages | 200 mg/kg |
| Administration | oral gavage |
| 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.
| Molecular Weight | 328.37 |
| Formula | C20H16N4O |
| CAS Number | 2288709-96-4 |
| Purity | >99% |
| Solubility | DMSO 70 mg/mL |
| Storage | at -20°C |
| Related ATM/ATR Products |
|---|
| KU-60019
KU-60019 is an improved ATM kinase-specific inhibitor with IC50 of 6.3 nM. |
| Elimusertib hydrochloride
Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. |
| Gartisertib
Gartisertib (VX-803) is an ATP-competitive, orally active, selective ATR inhibitor with Ki<150 pM. Gartisertib inhibits atR-driven phosphorylation of checkpoint kinase-1 (Chk1) with an IC50 value of 8 nM. It has antitumor activity. |
| RP-3500
RP-3500 (ATR inhibitor 4) is an orally potent, selective ATR kinase inhibitor (ATRi) in biochemical assays IC50 1.00 nM. The RP-3500 is 30 times more selective to ATR (IC).50=120 nM), which is 2,000 times > ATM, DNA-PK, and PI3Kα kinase. |
| AZD0156
AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits ATM mediated signal transduction, prevents DNA damage checkpoint activation, damages DNA damage repair, and induces tumor cell apoptosis. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.
