WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205841
CAS#: 1657014-42-0 (2HCl)
Description: GDC-0575, also known as ARRY-575 and RG7741, is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. Chk1 inhibitor GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis.
MedKoo Cat#: 205841
Name: GDC0575 dihydrochloride
CAS#: 1657014-42-0 (2HCl)
Chemical Formula: C16H22BrCl2N5O
Molecular Weight: 451.19
Elemental Analysis: C, 42.59; H, 4.92; Br, 17.71; Cl, 15.71; N, 15.52; O, 3.55
This product is not in stock, which may be available by custom synthesis.
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Synonym: GDC-0575; GDC 0575; GDC0575; ARRY-575; ARRY-575; ARRY575; RG7741; RG-7741; RG 7741; AK 687476; AK-687476; AK687476; GDC-0575 HCl; GDC-0575 hydrochloride
IUPAC/Chemical Name: (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide dihydrochloride
InChi Key: OYMHZTORKRPOBI-YQFADDPSSA-N
InChi Code: InChI=1S/C16H20BrN5O.2ClH/c17-11-6-19-15-13(14(11)22-5-1-2-10(18)8-22)12(7-20-15)21-16(23)9-3-4-9;;/h6-7,9-10H,1-5,8,18H2,(H,19,20)(H,21,23);2*1H/t10-;;/m1../s1
SMILES Code: O=C(C1CC1)NC2=CNC3=C2C(N4C[C@H](N)CCC4)=C(Br)C=C3.[H]Cl.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 451.19 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Grellety T, Callens C, Richard E, Briaux A, Vélasco V, Pulido M, Gonçalvès A, Gestraud P, MacGrogan G, Bonnefoi H, Cardinaud B. Enhancing abiraterone acetate efficacy in androgen receptor-positive triple negative breast cancer: Chk1 as a potential target. Clin Cancer Res. 2018 Oct 23. pii: clincanres.1469.2018. doi: 10.1158/1078-0432.CCR-18-1469. [Epub ahead of print] PubMed PMID: 30352905.
2: Italiano A, Infante JR, Shapiro GI, Moore KN, LoRusso PM, Hamilton E, Cousin S, Toulmonde M, Postel-Vinay S, Tolaney S, Blackwood EM, Mahrus S, Peale FV, Lu X, Moein A, Epler J, DuPree K, Tagen M, Murray ER, Schutzman JL, Lauchle JO, Hollebecque A, Soria JC. Phase I study of the checkpoint kinase 1 inhibitor GDC-0575 in combination with gemcitabine in patients with refractory solid tumors. Ann Oncol. 2018 Feb 23. doi: 10.1093/annonc/mdy076. [Epub ahead of print] PubMed PMID: 29788155.
3: Oo ZY, Stevenson AJ, Proctor M, Daignault SM, Walpole S, Lanagan C, Chen J, Škalamera D, Spoerri L, Ainger SA, Sturm RA, Haass NK, Gabrielli B. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Jun 15;24(12):2901-2912. doi: 10.1158/1078-0432.CCR-17-2701. Epub 2018 Mar 13. PubMed PMID: 29535131.
4: Laroche-Clary A, Lucchesi C, Rey C, Verbeke S, Bourdon A, Chaire V, Algéo MP, Cousin S, Toulmonde M, Vélasco V, Shutzman J, Savina A, Le Loarer F, Italiano A. CHK1 inhibition in soft-tissue sarcomas: biological and clinical implications. Ann Oncol. 2018 Apr 1;29(4):1023-1029. doi: 10.1093/annonc/mdy039. PubMed PMID: 29409053.
5: Di Tullio A, Rouault-Pierre K, Abarrategi A, Mian S, Grey W, Gribben J, Stewart A, Blackwood E, Bonnet D. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia. Nat Commun. 2017 Nov 22;8(1):1679. doi: 10.1038/s41467-017-01834-4. PubMed PMID: 29162833; PubMed Central PMCID: PMC5698422.