1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)

GDC-0575 (Synonyms: ARRY-575, RG7741)

Cat. No.: HY-112167 Purity: >98.0%
Handling Instructions

GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.

For research use only. We do not sell to patients.

GDC-0575 Chemical Structure

GDC-0575 Chemical Structure

CAS No. : 1196541-47-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 264 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
10 mg USD 380 In-stock
Estimated Time of Arrival: December 31
25 mg USD 780 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • References

Description

GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.

IC50 & Target

1.2 nM (Chk1)[1]

In Vitro

GDC-0575 is significantly more potent in promoting DNA damage, replication stress and cell death than V158411, LY2603618, and MK-8776 in a panel of melanoma cell lines[1]. GDC-0575 abrogates DNA damage-induced S and G2–M checkpoints, exacerbates DNA double-strand breaks and induces apoptosis in STS cells. GDC-0575 has a synergistic or additive effect together with gemcitabine[2]. CHK1 inhibitor GDC-0575 in combination with AraC enhances the killing of primary acute myeloid leukemia cells ex vivo by inducing apoptosis[3].

In Vivo

GDC-0575 is active at 25 mg/kg as a single agent, but the efficacy is improved at the higher drug dose. GDC-0575 effectively blocks tumor growth in the D20 and C002 xenografts, and the effect is maintained for at least 10 days after the final dose is administered[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (132.18 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6436 mL 13.2181 mL 26.4361 mL
5 mM 0.5287 mL 2.6436 mL 5.2872 mL
10 mM 0.2644 mL 1.3218 mL 2.6436 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[3]

AML cell lines are seeded at 1×104 cells/well in 96-well plates in triplicate, and subjected to different treatment conditions. After 24 h of incubation with GDC-0575, cell proliferation is measured with the XTT Cell Proliferation Kit II[3].

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

Animal Administration
[1]

Mice[1]

Female nude BALB/c mice are injected with 2-3×106 melanoma cells in Matrigel by subcutaneous injection on the hind flank. Once tumors reach approximately 100 mm3, mice are treated with GDC-0575 (25 mg/kg, 50 mg/kg) or vehicle (0.5% w/v methylcellulose and 0.2%v/v Tween 80) by oral gavage for 3 cycles where one cycle is three consecutive days of treatment followed by four rest days. Tumor size is measured three times per week using calipers. Mice are sacrificed at up to 6 weeks after terminating the treatment or when tumor size measured >1 cm3[1].

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

References
Molecular Weight

378.27

Formula

C₁₆H₂₀BrN₅O

CAS No.

1196541-47-5

SMILES

O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[[email protected]](N)CCC4)=C32

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GDC-0575
Cat. No.:
HY-112167
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GDC-0575

Cat. No.: HY-112167