2. Cell Cycle/DNA Damage
  3. Checkpoint Kinase (Chk)
  4. GDC-0575

GDC-0575  (Synonyms: ARRY-575; RG7741)

Cat. No.: HY-112167 Purity: 99.23%
COA Handling Instructions

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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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 In-stock
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 140 In-stock
10 mg USD 240 In-stock
25 mg USD 520 In-stock
50 mg USD 780 In-stock
100 mg USD 1170 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of GDC-0575:

GDC-0575 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

GDC-0575 Related Antibodies
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].

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

378.27

Formula

C16H20BrN5O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (264.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.50%

COA (256 KB) LCMS (272 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6436 mL 13.2181 mL 26.4361 mL 66.0904 mL
5 mM 0.5287 mL 2.6436 mL 5.2872 mL 13.2181 mL
10 mM 0.2644 mL 1.3218 mL 2.6436 mL 6.6090 mL
15 mM 0.1762 mL 0.8812 mL 1.7624 mL 4.4060 mL
20 mM 0.1322 mL 0.6609 mL 1.3218 mL 3.3045 mL
25 mM 0.1057 mL 0.5287 mL 1.0574 mL 2.6436 mL
30 mM 0.0881 mL 0.4406 mL 0.8812 mL 2.2030 mL
40 mM 0.0661 mL 0.3305 mL 0.6609 mL 1.6523 mL
50 mM 0.0529 mL 0.2644 mL 0.5287 mL 1.3218 mL
60 mM 0.0441 mL 0.2203 mL 0.4406 mL 1.1015 mL
80 mM 0.0330 mL 0.1652 mL 0.3305 mL 0.8261 mL
100 mM 0.0264 mL 0.1322 mL 0.2644 mL 0.6609 mL
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GDC-0575 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GDC-05751196541-47-5ARRY-575 RG7741GDC0575GDC 0575ARRY575ARRY 575RG7741RG 7741RG-7741Checkpoint Kinase (Chk)Inhibitorinhibitorinhibit

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