GDC-0425 free base
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MedKoo CAT#: 205840

CAS#: 1200129-48-1 (free base)

Description: GDC-0425, also known as RG 7602, is a Checkpoint Kinase 1 inhibitor. GDC-0425 selectively binds to chk1, thereby preventing activity of chk1 and abrogating the repair of damaged DNA. This may lead to an accumulation of damaged DNA, inhibition of cell cycle arrest, and induction of apoptosis. GDC-0425 may potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapeutic agents.


Chemical Structure

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GDC-0425 free base
CAS# 1200129-48-1 (free base)

Theoretical Analysis

MedKoo Cat#: 205840
Name: GDC-0425 free base
CAS#: 1200129-48-1 (free base)
Chemical Formula: C18H19N5O
Exact Mass: 321.16
Molecular Weight: 321.384
Elemental Analysis: C, 67.27; H, 5.96; N, 21.79; O, 4.98

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5mg USD 250 2 Weeks
10mg USD 450 2 Weeks
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Related CAS #: 1778671-05-8 (HCl)   1200129-48-1 (free base)    

Synonym: GDC0425; GDC-0425; GDC 0425; RG7602; RG-7602; RG 7602.

IUPAC/Chemical Name: 5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile

InChi Key: XEZLBMHDUXSICI-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H19N5O/c1-2-23-8-5-12(6-9-23)24-17-14(10-19)21-11-15-16(17)13-4-3-7-20-18(13)22-15/h3-4,7,11-12H,2,5-6,8-9H2,1H3,(H,20,22)

SMILES Code: N#CC1=NC=C2C(C3=CC=CN=C3N2)=C1OC4CCN(CC)CC4

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

More Info:         

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 321.38 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Takahashi RH, Halladay JS, Siu M, Chen Y, Hop CE, Khojasteh SC, Ma S. Novel Mechanism of Decyanation of GDC-0425 by Cytochrome P450. Drug Metab Dispos. 2017 May;45(5):430-440. doi: 10.1124/dmd.116.074336. Epub 2017 Feb 10. PMID: 28188299.


2: Lee HJ, Cao Y, Pham V, Blackwood E, Wilson C, Evangelista M, Klijn C, Stokoe D, Settleman J. Ras-MEK Signaling Mediates a Critical Chk1-Dependent DNA Damage Response in Cancer Cells. Mol Cancer Ther. 2017 Apr;16(4):694-704. doi: 10.1158/1535-7163.MCT-16-0504. Epub 2017 Jan 30. PMID: 28138032.


3: Infante JR, Hollebecque A, Postel-Vinay S, Bauer TM, Blackwood EM, Evangelista M, Mahrus S, Peale FV, Lu X, Sahasranaman S, Zhu R, Chen Y, Ding X, Murray ER, Schutzman JL, Lauchle JO, Soria JC, LoRusso PM. Phase I Study of GDC-0425, a Checkpoint Kinase 1 Inhibitor, in Combination with Gemcitabine in Patients with Refractory Solid Tumors. Clin Cancer Res. 2017 May 15;23(10):2423-2432. doi: 10.1158/1078-0432.CCR-16-1782. Epub 2016 Nov 4. PMID: 27815358.


4: Ding X, Chen Y, Sahasranaman S, Shi Y, McKnight J, Dean B. A supported liquid extraction LC-MS/MS method for determination of concentrations of GDC-0425, a small molecule Checkpoint kinase 1 inhibitor, in human plasma. Biomed Chromatogr. 2016 Dec;30(12):1984-1991. doi: 10.1002/bmc.3775. Epub 2016 Jul 5. PMID: 27245274.