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897016-82-9 (KX2-391)

1

Identification

KX2-391 KX2-391
Name KX2-391
Formula C26H29N3O3
MW 431.53
CAS No. 897016-82-9
EINECS
Smiles O=C(CC1=NC=C(C2=CC=C(OCCN3CCOCC3)C=C2)C=C1)NCC4=CC=CC=C4
Synonyms KX 01;KX 2-391;KX01;KX-01; N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide
InChI InChI=1S/C26H29N3O3/c30-26(28-19-21-4-2-1-3-5-21)18-24-9-6-23(20-27-24)22-7-10-25(11-8-22)32-17-14-29-12-15-31-16-13-29/h1-11,20H,12-19H2,(H,28,30)
2

Introduction

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.

Background Information

KX2-391 is a synthetic, orally bioavailable small molecule and non-ATP competitive Src tyrosine kinase signaling inhibitor with an IC50 of average 72 nM. KX2-391 has potential antineoplastic activity. Src kinase inhibitor KX2-391 specifically binds to the peptide substrate binding site of Src kinase. In addition, KX2-391 also inhibits microtubule polymerization. Preclinical studies have suggested that KX2-391 is able to prevent the proliferation and metastasis of prostate cancer cell lines in mouse xenografts. KX2-391 phase I clinical trials have been completed. ......by AbMole BioScience

KX2-391 is a novel non-ATP competitive substrate-pocket directed SRC inhibitor.

......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
KX2-391 is an orally bioavailable small molecule Src kinase inhibitor with potential antineoplastic activity. Unlike other Src kinase inhibitors which bind to the ATP-binding site, Src kinase inhibitor KX2-391 specifically binds to the peptide substrate b ......by BOC Sciences
KX2-391 is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. ......by MedChemexpress Co., Ltd.
Tirbanibulin, also known as KX-01, is the first clinical Src inhibitor of the novel peptidomimetic class that targets the peptide substrate site of Src providing more specificity toward Src kinase. ......by MedKoo Biosciences, Inc.
KX2-391(Tirbanibulin, KX 01, KX 2-391) is a highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor; inhibits c-Src kinase with GI50s of 1.34 uM and 2.30 μM in NIH3T3/c-Src527F and SYF/c-Src527F cells, respectively; causes microtubule disruption in tumor cells; orally active.Solid TumorsPhase 2 Clinical ......by ProbeChem
KX2-391, 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 2. ......by Selleck Chemicals LLC
KX2-391, 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 2. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Cell lines Huh7, PLC/PRF/5, Hep3B, and HepG2 cell lines
Conditions 6,564 to 0.012 nM; 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.</
Source Selleck Chemicals LLC

Animal Experiment

4

Physical and Chemical Properties

Appearance: EBNumber:EB000028918

Storage condition

Solubility

DMSO ≥82mg/mL Water <1.2mg/mL Ethanol ≥10mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 86 mg/mL (199.29 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM); In vivo 4% DMSO+30% PEG 300+ddH2O5mg/mL by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
KX2-391 Kinex Pharmaceuticals Corp Hormone refractory prostate cancer 2010/2/28 2012/8/31 Phase 2 Clinical
KX2-391 Hanmi Pharmaceutical Co Ltd Advanced solid tumor 2012/12/31 2016/5/31 Phase 2 Clinical
KX2-391 Kinex Pharmaceuticals Corp Acute myelogenous leukemia 2011/7/31 2013/10/31 Phase 1 Clinical
KX2-391 Kinex Pharmaceuticals Corp Lymphoma 2007/11/30 2011/5/31 Phase 1 Clinical
KX2-391 Kinex Pharmaceuticals Corp Solid tumor 2007/11/30 2011/5/31 Phase 1 Clinical
KX2-391 - Phase 2
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Safety Data of KX2-391

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD84();10mg/USD144() USA
Cayman Chemical Company USA
MedChemexpress Co., Ltd. 5mg/USD84();10mg/USD144() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Selleck Chemicals LLC 5mg/USD90(In stock);10mM/1mLIn DMSO/USD160(In stock);10mg/USD170(In stock);50mg/USD570(In stock);100mg/USD970(In stock);200mg/USD1670(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD84();10mg/USD144() China
Target Molecule Corp. 2mg/USD51();5mg/USD99();10mg/USD170();25mg/USD283();50mg/USD435() USA
10

Related Products

Other Forms of 897016-82-9

Name CAS No Formula MW
KX2-391 (dihydrochloride) 1038395-65-1 C26H31Cl2N3O3 504.45
KX2-391 (Mesylate) 1080645-95-9 C27H33N3O6S 527.6324

Recommended Compounds in Src Microtubule/Tubulin

Name CAS No Formula MW
Scutellarein 529-53-3 C15H10O6 286.24
A 419259 (trihydrochloride) 1435934-25-0 C29H37Cl3N6O 592.0
A 419259 364042-47-7 C29H34N6O 482.62
1-Naphthyl PP1 221243-82-9 C19H19N5 317.39
XL228 898280-07-4 C22H31N9O 437.54
Dasatinib (hydrochloride) 854001-07-3 C22H27Cl2N7O2S 524.47
MNS 1485-00-3 C9H7NO4 193.15618
PP2 172889-27-9 C15H16ClN5 301.77
PP1 172889-26-8 C16H19N5 281.36
ZM 306416 690206-97-4 C16H13ClFN3O2 333.74
AMG-47a 882663-88-9 C29H28F3N5O2 535.56
KX1-004 518058-84-9 C16H13FN2O2 284.29
AZM475271 476159-98-5 C23H27ClN4O3 442.9385
DCC-2036 1020172-07-9 C30H28FN7O3 553.59
Lck Inhibitor 847950-09-8 C31H30N8O 530.62
Lck inhibitor 2 944795-06-6 C18H17N5O2 335.36
PD173955 260415-63-2 C21H16Cl2N4OS 443.35
TG 100801 (Hydrochloride) 1018069-81-2 C33H31Cl2N5O3 616.54
TG 100801 867331-82-6 C33H30ClN5O3 580.08
TG 100572 (Hydrochloride) 867331-64-4 C26H27Cl2N5O2 512.43

Recommended Compounds in Same Indication

Name CAS No Formula MW
AZD1152 722543-31-9 C26H31FN7O6P 587.54
AZD1152-HQPA 722544-51-6 C26H30FN7O3 507.56
Mocetinostat 726169-73-9 C23H20N6O 396.44
OSI-930 728033-96-3 C22H16F3N3O2S 443.44
TAK-700 (R-form) 752243-39-3 C18H17N3O2 307.35
Volasertib 755038-65-4 C34H50N8O3 618.81
Olaparib 763113-22-0 C24H23FN4O3 434.46
AT7867 857531-00-1 C20H20ClN3 337.85
NVP-BGJ398 872511-34-7 C26H31Cl2N7O3 560.48
PU-H71 873436-91-0 C18H21IN6O2S 512.37
BMS-599626 (Hydrochloride) 873837-23-1 C27H28ClFN8O3 567.01
RO4987655 874101-00-5 C20H19F3IN3O5 565.28
MGCD-265 analog 875337-44-3 C26H20FN5O2S2 517.5977
Regorafenib (Hydrochloride) 835621-07-3 C21H16Cl2F4N4O3 519.28
AT9283 896466-04-9 C19H23N7O2 381.43
Bicalutamide 90357-06-5 C18H14F4N2O4S 430.37
Bleomycin (sulfate) 9041-93-4 C110H168N34O46S7 2927.17
MLN4924 905579-51-3 C21H25N5O4S 443.52
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
Enzalutamide 915087-33-1 C21H16F4N4O2S 464.44
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Route of Synthesis

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References

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More Information

KX2-391

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