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GDC-0575 (ARRY-575)

Cat. No. M10476
GDC-0575 (ARRY-575) Structure
Synonym:

RG7741; ARRY575; AK-687476

Size Price Availability Quantity
5mg USD 220  USD220 In stock
10mg USD 340  USD340 In stock
25mg USD 600  USD600 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 378.27
Formula C16H20BrN5O
CAS Number 1196541-47-5
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

[1] A Italiano, et al. Ann Oncol. Phase I study of the checkpoint kinase 1 inhibitor GDC-0575 in combination with gemcitabine in pаtιепts with refractory solid tumors

[2] Zay Yar Oo, et al. Clin Cancer Res. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo

[3] A Laroche-Clary, et al. Ann Oncol. CHK1 inhibition in soft-tissue sarcomas: biological and clinical implications

[4] Alessandro Di Tullio, et al. Nat Commun. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia

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  Catalog
Abmole Inhibitor Catalog




Keywords: GDC-0575 (ARRY-575), RG7741; ARRY575; AK-687476 supplier, Checkpoint, inhibitors

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