LQZ-7I
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    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.

Chemical Structure

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LQZ-7I
CAS# 195822-23-2
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 408100
Name: LQZ-7I
CAS#: 195822-23-2
Chemical Formula: C20H14F2N4
Exact Mass: 348.12
Molecular Weight: 348.357
Elemental Analysis: C, 68.96; H, 4.05; F, 10.91; N, 16.08

Price and Availability

Size Price Availability Quantity
10mg USD 110 Ready to ship
25mg USD 190 Ready to ship
50mg USD 350 Ready to ship
100mg USD 550 Ready to ship
200mg USD 950 Ready to ship
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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

More Info: 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.

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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 5.0 14.35
DMSO 2.0 5.74
Ethanol 1.0 2.87

Preparing Stock Solutions

The following data is based on the product molecular weight 348.36 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.

Recalculate based on batch purity %
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.

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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