GDC-0575 freebase
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MedKoo CAT#: 584642

CAS#: 1196541-47-5 (free base)

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.


Price and Availability

Size
Price

500mg
USD 2950
Size
Price

1g
USD 3850
Size
Price

2g
USD 6650

GDC-0575 free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 584642
Name: GDC-0575 freebase
CAS#: 1196541-47-5 (free base)
Chemical Formula: C16H20BrN5O
Exact Mass: 377.0851
Molecular Weight: 378.274
Elemental Analysis: C, 50.80; H, 5.33; Br, 21.12; N, 18.51; O, 4.23


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

InChi Key: BAZRWWGASYWYGB-SNVBAGLBSA-N

InChi Code: InChI=1S/C16H20BrN5O/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)/t10-/m1/s1

SMILES Code: O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[C@H](N)CCC4)=C32


Technical Data

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

Shelf Life:
>3 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).

Harmonized System Code:
2934990300


References

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.