GDC0575 hydrochloride  (Synonyms: ARRY-575 hydrochloride; RG7741 hydrochloride)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

414.73

C₁₆H₂₁BrClN₅O

1196504-54-7

O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[C@H](N)CCC4)=C32.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]