Synonym
GDC-0134; GDC0134; GDC 0134; RG-6000; RG6000; RG 6000
IUPAC/Chemical Name
5-(6-((1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)-2-(3,3-difluoropyrrolidin-1-yl)pyrimidin-4-yl)-3-(difluoromethoxy)pyridin-2-amine
InChi Key
SKMKJBYBPYBDMN-RYUDHWBXSA-N
InChi Code
InChI=1S/C19H20F4N6O2/c20-17(21)31-14-3-10(6-25-16(14)24)13-5-15(29-7-12-4-11(29)8-30-12)27-18(26-13)28-2-1-19(22,23)9-28/h3,5-6,11-12,17H,1-2,4,7-9H2,(H2,24,25)/t11-,12-/m0/s1
SMILES Code
NC1=NC=C(C2=NC(N3CC(F)(F)CC3)=NC(N4[C@]5([H])CO[C@](C5)([H])C4)=C2)C=C1OC(F)F
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
440.40
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. Katz JS, Rothstein JD, Cudkowicz ME, Genge A, Oskarsson B, Hains AB, Chen C, Galanter J, Burgess BL, Cho W, Kerchner GA, Yeh FL, Ghosh AS, Cheeti S, Brooks L, Honigberg L, Couch JA, Rothenberg ME, Brunstein F, Sharma KR, van den Berg L, Berry JD, Glass JD. A Phase 1 study of GDC-0134, a dual leucine zipper kinase inhibitor, in ALS. Ann Clin Transl Neurol. 2022 Jan;9(1):50-66. doi: 10.1002/acn3.51491. Epub 2022 Jan 10. PMID: 35014217; PMCID: PMC8791798.
2. https://genentech-clinicaltrials.com/en/trials/neurodegenerative-disorder/als/a-study-of-gdc-0134-to-determine-initial-safety--tolerability--a.html