SGX-523

Name: SGX-523
Brand: MedChemExpress
SKU: HY-12019
Rating: 5.0 (7 reviews)

Cat. No.: HY-12019 Purity: ≥99.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC₅₀ of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity.

For research use only. We do not sell to patients.

SGX-523 Chemical Structure

CAS No. : 1022150-57-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 295	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 470	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

6 Publications Citing Use of MCE SGX-523

: SGX-523 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2015 Nov 1;75(21):4548-59. [Abstract]; c-Myc downregulation is essential for c-Met inhibition caused by growth arrest in MET-addicted cells. EBC-1, NCI-H1993, SNU-5, MKN-45, and HCC827 cells are treated with SGX-523 at 1 μM for 24 or 48 hours followed by immunoblotting analysis of cell-cycle regulators.

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 10000 nM Compound: 1; SGX-523	Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
HCCLM3	IC₅₀	24 nM Compound: 1; SGX-523	Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
Huh-7	IC₅₀	> 10000 nM Compound: 1; SGX-523	Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
MHCC97H	IC₅₀	11 nM Compound: 1; SGX-523	Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
MKN-45	IC₅₀	15 nM Compound: 1; SGX-523	Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
NCI-H1975	IC₅₀	> 10000 nM Compound: 1; SGX-523	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
NCI-H1993	IC₅₀	25 nM Compound: 1; SGX-523	Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
NCI-N87	IC₅₀	> 10000 nM Compound: 1; SGX-523	Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
SNU-5	IC₅₀	3.9 nM Compound: 1; SGX-523	Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]

In Vitro

SGX523 shows ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), K_i=2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), K_i=23 nM]^[1].
SGX523 inhibits the growth of gastric and lung cancer cell lines with amplification of the MET gene but has no effect, even at high micromolar concentration, on cell lines with normal MET gene copy number. TheIC₅₀s of 0.02, 0.113, and 0.035 μM for NSCLC H1993, gastric cncer MKN45, and gastric cancer Hs746T cells, respectively^[1].
The IC₅₀ value for the inhibition of MET autophosphorylation is 0.040 μM in GTL16 cells^[1].
SGX523 (0.5, 1.5, 4.6, 13.7, 41, 123, 370, 1100, 3300, 10000 nM; 1 hour) inhibits MET autophosphorylation without affecting total MET or extracellular signal-regulated kinase protein levels in HGF-stimulated A549 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	Gastric cancer cell line GTL16
Concentration:	4.6, 14, 40, 120, 370, 1100, 3300, 10000 nM
Incubation Time:	1 hours
Result:	Abolished constitutive signaling induced by MET gene amplification.

In Vivo

SGX523 exhibits antitumor activity in vivo. SGX523 inhibits MET-dependent tumor growth^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Harlan nude mice (athymic nu/nu) were s.c. implanted with U87 cells^[2]
Dosage:	10 or 30 mg/kg
Administration:	Oral gavage; twice daily starting at day 5 for 22 days
Result:	Potently inhibited U87MG tumor growth at a dose of 10 mg/kg administered twice daily. Led to clear regression of U87MG tumors at 30 mg/kg dosed twice daily.

Clinical Trial

Molecular Weight

359.41

Formula

C₁₈H₁₃N₇S

CAS No.

1022150-57-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

CN1N=CC(C2=NN3C(SC4=CC5=C(N=CC=C5)C=C4)=NN=C3C=C2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 30 mg/mL (83.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7823 mL	13.9117 mL	27.8234 mL
5 mM	0.5565 mL	2.7823 mL	5.5647 mL
10 mM	0.2782 mL	1.3912 mL	2.7823 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

SGX-523 is prepared in 0.5% sodium carboxymethyl cellulose^[2].

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: ≥99.0%

Select Batch:

Data Sheet (277 KB) SDS (392 KB)

COA (252 KB) HNMR (86 KB)

Handling Instructions (2659 KB)

References

[1]. Buchanan SG, et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther, 2009, 8(12), 3181-3190. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7823 mL	13.9117 mL	27.8234 mL	69.5584 mL
	5 mM	0.5565 mL	2.7823 mL	5.5647 mL	13.9117 mL
	10 mM	0.2782 mL	1.3912 mL	2.7823 mL	6.9558 mL
	15 mM	0.1855 mL	0.9274 mL	1.8549 mL	4.6372 mL
	20 mM	0.1391 mL	0.6956 mL	1.3912 mL	3.4779 mL
	25 mM	0.1113 mL	0.5565 mL	1.1129 mL	2.7823 mL
	30 mM	0.0927 mL	0.4637 mL	0.9274 mL	2.3186 mL
	40 mM	0.0696 mL	0.3478 mL	0.6956 mL	1.7390 mL
	50 mM	0.0556 mL	0.2782 mL	0.5565 mL	1.3912 mL
	60 mM	0.0464 mL	0.2319 mL	0.4637 mL	1.1593 mL
	80 mM	0.0348 mL	0.1739 mL	0.3478 mL	0.8695 mL

SGX-523 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SGX-5231022150-57-7SGX523SGX 523c-Met/HGFRexquisitelyselectiveMETantitumorInhibitorinhibitorinhibit

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SGX-523

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SGX-523 Related Antibodies

6 Publications Citing Use of MCE SGX-523

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Complete Stock Solution Preparation Table

SGX-523 Related Classifications

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