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
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
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.
| 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 |
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.
