WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H122443
CAS#: N/A
Description: ZJH-16 is an EED−H3K27me3 Inhibitor for the Treatment of Lymphoma. ZJH-16 directly binds to EED (HTRF IC50 = 2.72 nM, BLI KD = 4.4 nM) and potently inhibits the growth of KARPAS422 and Pfeiffer cells. In both cells, ZJH-16 is selectively engaged with EED and reduces H3K27 trimethylation levels. ZJH-16 inhibits the gene silencing function of PRC2 in KARPAS422 cells. ZJH-16 possesses favorable pharmacokinetic (PK) profiles with an excellent oral bioavailability (F =94.7%). More importantly, ZJH-16 shows robust tumor regression in the KARPAS422 xenograft model after oral administration with the tumor growth inhibition reaching nearly 100%.
Hodoodo Cat#: H122443
Name: ZJH-16
CAS#: N/A
Chemical Formula: C18H14N6O
Exact Mass: 330.12
Molecular Weight: 330.350
Elemental Analysis: C, 65.44; H, 4.27; N, 25.44; O, 4.84
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Synonym: ZJH-16, ZJH16, ZJH 16
IUPAC/Chemical Name: N-(furan-2-ylmethyl)-8-(1H-indol-7-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine
InChi Key: QIEWQHLMHMLRBF-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H14N6O/c1-3-12-6-7-19-16(12)14(5-1)15-10-21-18(24-11-22-23-17(15)24)20-9-13-4-2-8-25-13/h1-8,10-11,19H,9H2,(H,20,21)
SMILES Code: C12=CC=CC(C3=CN=C(NCC4=CC=CO4)N5C3=NN=C5)=C1NC=C2
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 330.35 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: |
Dong G, Zuo J, Yu J, Xu J, Gao G, Li GB, Zhao W, Yu B. Structure-Based Design of the Indole-Substituted Triazolopyrimidines as New EED-H3K27me3 Inhibitors for the Treatment of Lymphoma. J Med Chem. 2022 Dec 29. doi: 10.1021/acs.jmedchem.2c02028. Epub ahead of print. PMID: 36580346.