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Chemical Structure| 1196541-47-5 Chemical Structure| 1196541-47-5

Structure of GDC-0575
CAS No.: 1196541-47-5

Chemical Structure| 1196541-47-5

GDC-0575

CAS No.: 1196541-47-5

GDC-0575 is a potent and selective CHK1 inhibitor.

Synonyms: ARRY-575; RG7741

4.5 *For Research Use Only !

Cat. No.: A690852 Purity: 98+%

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Product Details of GDC-0575

CAS No. :1196541-47-5
Formula : C16H20BrN5O
M.W : 378.27
SMILES Code : O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[C@H](N)CCC4)=C32
Synonyms :
ARRY-575; RG7741
MDL No. :MFCD29048675
InChI Key :BAZRWWGASYWYGB-SNVBAGLBSA-N
Pubchem ID :46917793

Safety of GDC-0575

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary AML cells 100 nM 1 week To study the killing effect of GDC-0575 in combination with AraC on primary AML cells. Results showed that the combination treatment significantly reduced AML cell survival but had little effect on the frequency of long-term culture-initiating cells (L-LTC-IC). Nat Commun. 2017 Nov 22;8(1):1679.
AML cell lines (HL60, KG-1, ML1, U937) 100 nM 24 hours To evaluate the cytotoxic and apoptosis-inducing effects of GDC-0575 in combination with AraC on AML cell lines. Results showed that GDC-0575 significantly enhanced the killing effect of AraC on AML cells and increased apoptosis. Nat Commun. 2017 Nov 22;8(1):1679.
N2a/APP cells 0.2, 0.5, 1 μM 24 hours GDC-0575 dose-dependently reduced Chk1 protein levels, significantly decreased CIP2A levels and tau phosphorylation (at Ser199, Ser396, and AT8 sites) and APP levels Neurotherapeutics. 2022 Mar;19(2):570-591.
HEK293/tau cells 0.2, 0.5, 1 μM 24 hours GDC-0575 dose-dependently reduced Chk1 protein levels, significantly decreased CIP2A levels and tau phosphorylation (at Ser199, Ser396, and AT8 sites) and APP levels Neurotherapeutics. 2022 Mar;19(2):570-591.
TC71 cells 1 μM 4 hours To evaluate the effect of GDC-0575 on TC71 cell growth, results showed that GDC-0575 significantly inhibited cell growth. Mol Cancer Res. 2020 Jan;18(1):91-104.
EW8 cells 1 μM 4 hours To evaluate the effect of GDC-0575 on EW8 cell growth, results showed that GDC-0575 significantly inhibited cell growth. Mol Cancer Res. 2020 Jan;18(1):91-104.
U2OS cells 300 nM Used to study the role of ATR and CHK1 in transcriptional inhibition induced by rDNA breaks Nat Commun. 2020 Jan 8;11(1):123.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice AML xenograft model Oral gavage 7.5 mg/kg Every other day for 7 days To evaluate the therapeutic effect of GDC-0575 in combination with AraC on AML xenograft models. Results showed that the combination treatment significantly reduced leukemic burden and delayed disease relapse. Additionally, the combination did not generate new mutations and may prevent the survival of AraC-induced mutagenic clones. Nat Commun. 2017 Nov 22;8(1):1679.
C57 mice DSS-induced acute colitis model and AOM/DSS-induced CAC model Oral 7.5 mg/kg Administered on days 15, 17, 19, and 21 post AOM injection GDC-0575 significantly inhibited CHK1 expression in the colon and dramatically impaired the development of CAC and colitis in mice. Moreover, the inhibition of CHK1 expression resulted in efficient inhibition of infiltration by iNOS-positive macrophages, but had no significant effect on CD4 T cells, CD8 T cells, and myeloid-derived suppressor cells (MDSCs). Significant downregulation of TNF-α, IL-6, and IL-1β and dramatic upregulation of IL-10 were observed in the colons of both mice with CAC and colitis treated with GDC-0575. CCL2 expression was also downregulated by GDC-0575 in both mice with CAC and colitis; this was followed by the inhibition of CCR2+ macrophage infiltration in the colon. Onco Targets Ther. 2021 Apr 15;14:2661-2672
APP/PS1 transgenic mice Alzheimer's disease model Oral gavage 25 mg/kg Twice a week for 3 weeks GDC-0575 treatment significantly inhibited Chk1 activity in the brains of APP/PS1 mice, reversed CIP2A upregulation, tau hyperphosphorylation and Aβ overproduction, ameliorated cognitive deficits, and prevented neuron loss and synaptic impairments Neurotherapeutics. 2022 Mar;19(2):570-591.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.22mL

2.64mL

1.32mL

26.44mL

5.29mL

2.64mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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