MedChemExpress - Model GDC0575 hydrochloride -1196504-54-7
GDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active Chk1 (IC50=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used for colitis-associated cancer (CAC) and colitis research[1].MCE products for research use only. We do not sell to patients.
GDC0575 hydrochloride
MCE China：GDC0575 hydrochloride
Brand：MedChemExpress (MCE)
Cat. No.HY-112167B
CAS：1196504-54-7
Synonyms：ARRY-575 hydrochloride; RG7741 hydrochloride
Storage：Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping：Room temperature in continental US; may vary elsewhere.
Description：GDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active Chk1 (IC50=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used for colitis-associated cancer (CAC) and colitis research.
In Vitro：GDC-0575 dihydrochloride is a selective and orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM. GDC-0575 (100 nM) suppressses CHK1 activation induced by AraC by decreasing the level of Tyr15-phosphorylated CDK2[1]. GDC-0575 dihydrochloride (100 nM) has no effect on the viability of AML cells, but significantly reduces cell viability and induces apoptosis in combination with AraC. GDC-0575 plus AraC shows no effect on normal hematopoietic stem and progenitor cells (HSPCs)[1]. GDC-0575 shows cytotoxic activity against most of 20 melanoma cell lines tested, but several cell lines grown as tumour sphere (TS) are relatively insensitive[2].
In Vivo：GDC-0575 dihydrochloride (7.5 mg/kg, p.o.) in combination with AraC alomost completely eradicates leukemic burden in mice transplanted with U937-Luc cells, and shows more efficient activity than AraC alone. GDC-0575 dihydrochloride elevates the cytotoxicity of AraC in different primary AML models in vivo[1]. GDC-0575 dihydrochloride (25, 50 mg/kg, p.o.) dose-dependently inhibits the growth of tumor in D20 and C002 xenografts[2].
IC50 & Target：Chk1 1.2 nM (IC50)
Hot selling product：2'-Deoxycytidine | Isocitric acid | DOTA-GA(tBu)4 | Acitretin | PD-1/PD-L1-IN-29 | Z-Nle-Lys-Arg-AMC (acetate) | Bafetinib | OTSSP167 | L-Thyroxine (sodium salt pentahydrate) | Ticlopidine
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
References：
[1]. Oo ZY, et al. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Mar 13. [Content Brief]
[2]. Laroche-Clary A, et al. CHK1 inhibition in soft-tissue sarcomas: biological and clinical implications. Ann Oncol. 2018 Apr 1;29(4):1023-1029. [Content Brief]
[3]. Di Tullio A, et al. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia. Nat Commun. 2017 Nov 22;8(1):1679. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
• It has a professional experimental center and strict quality control and verification system；
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
• The biological activity of the products has been verified by the experiments of customers in various countries；
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。