LQZ-7I | CAS#195822-23-2 | PfSUB1 inhibitor

MedKoo Cat#: 408100 | Name: LQZ-7I

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

LQZ-7I

CAS#195822-23-2

Theoretical Analysis

MedKoo Cat#: 408100

Name: LQZ-7I

CAS#: 195822-23-2

Chemical Formula: C20H14F2N4

Exact Mass: 348.1187

Molecular Weight: 348.36

Elemental Analysis: C, 68.96; H, 4.05; F, 10.91; N, 16.08

Price and Availability

Size	Price	Availability
10mg	USD 110.00	Ready to ship
25mg	USD 190.00	Ready to ship
50mg	USD 350.00	Ready to ship
100mg	USD 550.00	Ready to ship
200mg	USD 950.00	Ready to ship

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Related CAS #

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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.

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#T23D03P10

QC Data

View QC data: current batch, Lot#T23D03P10

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

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	mg/mL	mM
Solubility
	DMF	5.0	14.35
	DMSO	2.0	5.74
	Ethanol	1.0	2.87

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

In vivo protocol:

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