KX2-391

貨號 Cat. No.: S2700
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Description

KX2-391

Catalog No.S2700

KX2-391 (KX01), the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 1/2.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 201	In stock	0 1 2 3 4 5 6 7 8 9 10
5mg	USD 113	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 214	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 718	In stock	0 1 2 3 4 5 6 7 8 9 10
100mg	USD 1222	In stock	0 1 2 3 4 5 6 7 8 9 10
200mg	USD 2104	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Biological Activity

Description	KX2-391 (KX01), the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 1/2.
Targets	HuH7	PLC/PRF/5	Hep 3B	Hep G2
IC50	9 nM (GI50)	13 nM (GI50)	26 nM (GI50)	60 nM (GI50) ^[1]
In vitro	KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM), and HepG2 (GI 50 = 60 nM), four hepatic cell cancer (HCC) cell lines. ^[1] KX2-391 is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. KX2-391 is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively. ^[2]
In vivo	In pre-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis. ^[2]
Features

Protocol(Only for Reference)

Cell Assay:

^[1]

Cell lines	Huh7, PLC/PRF/5, Hep3B, and HepG2 cell lines
Concentrations	6,564 to 0.012 nM
Incubation Time	3 days
Method	Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 (NutriCyte, Buffalo, NY) are routinely cultured and maintained in basal medium containing 2% fetal bovine serum (FBS) at 37 °C and 5% CO₂. Cells are seeded at 4.0 × 10³/190 μL and 8.0 × 10³/190 μL per well of 96-well plate in basal medium containing 1.5% FBS. These are cultured overnight at 37 °C and 5% CO₂ prior to the addition of KX2-391, at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten microliters of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/mL) is then added to each well on day 3 and cells incubated for 4 hours. The formazan product is dissolved with 10% SDS in dilute HCl. Optical density at 570 nm is measured by using BioTek Synergy HT multiplatform microplate reader. For comparison of activity and potency, parallel experiments are performed using KX2-391. Growth inhibition curves, 50% inhibition concentration (GI50), and 80% inhibition concentration (GI80) are determined using GraphPad Prism 5 statistical software. Data are normalized to represent percentage of maximum response as well as reported in optical density at wavelength of 570 nm (OD570) signal format.

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT00646139	Completed	Lymphoma\|Lymphoproliferative Disorder\|Small Intestine Cancer\|Unspecified Adult Solid Tumor, Protocol Specific	Roswell Park Cancer Institute	2007-10	Phase 1
NCT00658970	Completed	Solid Tumors\|Lymphoma	Kinex Pharmaceuticals, LLC	2007-11	Phase 1
NCT01074138	Completed	Bone-Metastatic, Castration-Resistant Prostate Cancer	Kinex Pharmaceuticals, LLC	2010-02	Phase 2
NCT01397799	Active, not recruiting	Acute Myelogenous Leukemia	Kinex Pharmaceuticals, LLC	2011-07	Phase 1
NCT01764087	Recruiting	Unspecified Adult Solid Tumor, Protocol Specific\|Gastric Cancer\|Breast Cancer	Hanmi Pharmaceutical Company Limited	2012-12	Phase 1\|Phase 2

Chemical Information

Download KX2-391 SDF

Molecular Weight (MW)	431.53
Formula	C₂₆H₂₉N₃O₃
CAS No.	897016-82-9

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	86 mg/mL (199 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.