WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 408100
CAS#: 195822-23-2
Description: LQZ-7I is a malarial protease PfSUB1 inhibitor. LQZ-7I showed significantly improved activity and is the focus of this work. LQZ-7 when given orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors. The data obtained utilizing LQZ-7I in both in vitro and in vivo studies highlights its potential as a lead for further development, which may yield a potential cancer therapeutic by targeting the survivin protein directly.
MedKoo Cat#: 408100
Name: LQZ-7I
CAS#: 195822-23-2
Chemical Formula: C20H14F2N4
Exact Mass: 348.1187
Molecular Weight: 348.3568
Elemental Analysis: C, 68.96; H, 4.05; F, 10.91; N, 16.08
Synonym: LQZ-7I; LQZ 7I; LQZ7I;
IUPAC/Chemical Name: 2,3-Quinoxalinediamine, N,N'-bis(4-fluorophenyl)-
InChi Key: DKPCKOKYSVPFEB-UHFFFAOYSA-N
InChi Code: InChI=1S/C20H14F2N4/c21-13-5-9-15(10-6-13)23-19-20(24-16-11-7-14(22)8-12-16)26-18-4-2-1-3-17(18)25-19/h1-12H,(H,23,25)(H,24,26)
SMILES Code: FC1=CC=C(NC2=NC3=CC=CC=C3N=C2NC4=CC=C(F)C=C4)C=C1
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
Shelf Life: >3 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
| Biological target: | LQZ-7I is a survivin-targeting inhibitor. |
| In vitro activity: | As shown in Figure 5A,B, 7I induced cleavage of caspase 3 in a dose dependent manner in both cell lines. This study also performed annexin V staining of C4-2 and PC-3 cells as another indicator of apoptosis following 7I treatments. As shown in Figure 5C, 3 μM 7I induced ~48% and ~39% apoptosis in C4-2 and PC-3 cells, respectively. Reference: J Med Chem. 2020 Jul 9;63(13):7243-7251. https://pubmed.ncbi.nlm.nih.gov/32421328/ |
| In vivo activity: | As shown in Figure 6A, 7I treatment at 100 mg/kg significantly suppressed tumor growth without any notable adverse effect on the mice as indicated by lacking changes in body weight (Figure 6B) or in wet weight of major organs at the end of the study (Figure S4). The xenograft tumors in the 7I-teatment group tended to be smaller and paler in color than those of the control group (Figure 6C,,D).D). Thus, 7I may be effective in inhibiting tumor growth with little toxicity. Reference: J Med Chem. 2020 Jul 9;63(13):7243-7251. https://pubmed.ncbi.nlm.nih.gov/32421328/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 5.0 | 14.35 | |
| DMSO | 2.0 | 5.74 | |
| Ethanol | 1.0 | 2.87 |
The following data is based on the product molecular weight 348.3568 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: | Peery R, Kyei-Baffour K, Dong Z, Liu J, de Andrade Horn P, Dai M, Liu JY, Zhang JT. Synthesis and Identification of a Novel Lead Targeting Survivin Dimerization for Proteasome-Dependent Degradation. J Med Chem. 2020 Jul 9;63(13):7243-7251. doi: 10.1021/acs.jmedchem.0c00475. Epub 2020 Jun 9. PMID: 32421328; PMCID: PMC8216492. |
| In vitro protocol: | Peery R, Kyei-Baffour K, Dong Z, Liu J, de Andrade Horn P, Dai M, Liu JY, Zhang JT. Synthesis and Identification of a Novel Lead Targeting Survivin Dimerization for Proteasome-Dependent Degradation. J Med Chem. 2020 Jul 9;63(13):7243-7251. doi: 10.1021/acs.jmedchem.0c00475. Epub 2020 Jun 9. PMID: 32421328; PMCID: PMC8216492. |
| In vivo protocol: | Peery R, Kyei-Baffour K, Dong Z, Liu J, de Andrade Horn P, Dai M, Liu JY, Zhang JT. Synthesis and Identification of a Novel Lead Targeting Survivin Dimerization for Proteasome-Dependent Degradation. J Med Chem. 2020 Jul 9;63(13):7243-7251. doi: 10.1021/acs.jmedchem.0c00475. Epub 2020 Jun 9. PMID: 32421328; PMCID: PMC8216492. |
1. Peery, Robert; Kyei-Baffour, Kwaku; Dong, Zizheng; Liu, Jianguo; de Andrade Horn, Pedro; Dai, Mingji; Liu, Jing-Yuan; Zhang, Jian-Ting Synthesis and Identification of a Novel Lead Targeting Survivin Dimerization for Proteasome-Dependent Degradation, Journal of Medicinal Chemistry (2020), Ahead of Print
Survivin, a homodimeric member of the Inhibitor of Apoptosis Protein (IAP) family, is required for cancer cell survival and overexpressed in almost all solid tumors. However, targeting survivin has been challenging due to its “undruggable” nature.
