WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130458
CAS#: 1637394-01-4 (free base)
Description: GDC-0134 is a dual leucine zipper kinase (DLK) inhibitor with the ability to penetrate the brain. Inhibition of DLK prevents the degeneration of neurons and blocks the activation of JNK, serving as a potential treatment for ALS. GDC-0134 has undergone a phase 1 study for treating patients with amyotrophic lateral sclerosis (ALS).
Hodoodo Cat#: H130458
Name: GDC-0134
CAS#: 1637394-01-4 (free base)
Chemical Formula: C19H20F4N6O2
Exact Mass: 440.16
Molecular Weight: 440.403
Elemental Analysis: C, 51.82; H, 4.58; F, 17.26; N, 19.08; O, 7.27
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Related CAS #: 1637396-55-4 (isomer) 1637394-01-4 (free base) GDC0134 HCl
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
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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
