All AbMole products are for research use only, cannot be used for human consumption.
GDC-0575 (ARRY-575, RG7741) is a potent and selective oral inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. GDC-0575 abrogates DNA damage-induced S and G2–M checkpoints, exacerbates DNA double-strand breaks and induces apoptosis in STS cells. GDC-0575 has a synergistic or additive effect together with gemcitabine.
In vivo, GDC-0575 is active at 25 mg/kg as a single agent, but the efficacy is improved at the higher dose. GDC-0575 effectively blocks tumor growth in the D20 and C002 xenografts, and the effect is maintained for at least 10 days after the final dose is administered.
| Cell Experiment | |
|---|---|
| Cell lines | AML cell lines |
| Preparation method | AML cell lines are seeded at 1×104 cells/well in 96-well plates in triplicate, and subjected to different treatment conditions. After 24 h of incubation with GDC-0575, cell proliferation is measured with the XTT Cell Proliferation Kit II. |
| Concentrations | 100 nM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Female nude BALB/c mice |
| Formulation | 0.5% w/v methylcellulose and 0.2%v/v Tween 80 |
| Dosages | 25 mg/kg, 50 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 378.27 |
| Formula | C16H20BrN5O |
| CAS Number | 1196541-47-5 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Checkpoint Products |
|---|
| PV-1019
PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits IR-induced apoptosis. |
| CCT241533 dihydrochloride
CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM. |
| CBP501 Affinity Peptide
CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. |
| Chktide
Chktide is a substrate for CHK1 and CHK2. |
| Zn-DPA-maytansinoid conjugate 1
Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
