GDC0575 dihydrochloride

    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.


Chemical Structure

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GDC0575 dihydrochloride
CAS# 1657014-42-0 (2HCl)

Theoretical Analysis

MedKoo Cat#: 205841
Name: GDC0575 dihydrochloride
CAS#: 1657014-42-0 (2HCl)
Chemical Formula: C16H22BrCl2N5O
Exact Mass:
Molecular Weight: 451.19
Elemental Analysis: C, 42.59; H, 4.92; Br, 17.71; Cl, 15.71; N, 15.52; O, 3.55

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 1657014-42-0 (2HCl)   1196541-47-5 (free base)   1196504-54-7 (HCl)    

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

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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

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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.



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