2. Protein Tyrosine Kinase/RTK Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. Src Microtubule/Tubulin Apoptosis
  4. KX2-361

KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell.

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KX2-361

KX2-361 Chemische Struktur

CAS. Nr. : 897016-26-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO Auf Lager
Solid
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KX2-361 Related Antibodies

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Alle Src Isoform-spezifische Produkte anzeigen:

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Lck Fyn Blk Fgr Hck Lyn Yes Csk SRC-3

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Beschreibung

KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell[1].

Cellular Effect
Cell Line Type Value Description References
Daoy GI50
16 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human DaOY cells
Antiproliferative activity against human DaOY cells
[PMID: 29617135]
GL261 IC50
60 nM
Compound: 2; KX2-361; KX-02
Inhibition of Src autophosphorylation in mouse GL261 cells
Inhibition of Src autophosphorylation in mouse GL261 cells
[PMID: 29617135]
LN-18 GI50
2.9 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human LN18 cells
Antiproliferative activity against human LN18 cells
[PMID: 29617135]
SK-N-FI GI50
11 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human SK-N-FI cells
Antiproliferative activity against human SK-N-FI cells
[PMID: 29617135]
SK-N-MC GI50
8 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human SK-N-MC cells
Antiproliferative activity against human SK-N-MC cells
[PMID: 29617135]
SW1088 GI50
26 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human SW1088 cells
Antiproliferative activity against human SW1088 cells
[PMID: 29617135]
T98G GI50
14 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human T98G cells
Antiproliferative activity against human T98G cells
[PMID: 29617135]
U-118-MG GI50
29 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human U118MG cells
Antiproliferative activity against human U118MG cells
[PMID: 29617135]
U138-MG GI50
51 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human U138MG cells
Antiproliferative activity against human U138MG cells
[PMID: 29617135]
U-373MG ATCC GI50
54 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human U373 cells
Antiproliferative activity against human U373 cells
[PMID: 29617135]
U-87MG ATCC GI50
76 nM
Compound: 2; KX2-361; KX-02
Antiproliferative activity against human U87 cells
Antiproliferative activity against human U87 cells
[PMID: 29617135]
In Vitro

KX2-361 (0-200 nM, 24-72 h) reduces autophosphorylation of Src in GL261 cells[1].
KX2-361 (0-270 nM) promotes cell cycle arrest at the G2/M phase in U87 cells. Note the dose dependent effect and virtual complete arrest at 270 nM[1].
KX2-361 (0-800 nM) induces apoptosis of U87, GL261 and T98G cell lines[1].
KX2-361 (5 µM) inhibits the in vitro assembly of tubulin polymers[1].

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

KX2-361 Related Antibodies
In Vivo

KX2‑361 significantly delays progression of orthotopic GL261 brain tumors and produces long‑term survival[1].
KX2-361 demonstrates appreciable brain penetration when dosed orally to mice (20 mg/kg), with a brain Cmax of 4025±319 ng/g observed 15 min post-dosing and an overall exposure (AUClast) of 5044±355 h ng/g[1].

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

405.46

Formel

C24H24FN3O2
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1=CC=CC(F)=C1)CC2=NC=C(C3=CC=C(N4CCOCC4)C=C3)C=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 10.71 mg/mL (26.41 mM; ultrasonic and warming and heat to 60°C; 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 2.4663 mL 12.3317 mL 24.6633 mL
5 mM 0.4933 mL 2.4663 mL 4.9327 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
Reinheit & Dokumentation
Verweise

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4663 mL 12.3317 mL 24.6633 mL 61.6584 mL
5 mM 0.4933 mL 2.4663 mL 4.9327 mL 12.3317 mL
10 mM 0.2466 mL 1.2332 mL 2.4663 mL 6.1658 mL
15 mM 0.1644 mL 0.8221 mL 1.6442 mL 4.1106 mL
20 mM 0.1233 mL 0.6166 mL 1.2332 mL 3.0829 mL
25 mM 0.0987 mL 0.4933 mL 0.9865 mL 2.4663 mL
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KX2-361 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:

KX2-361897016-26-1KX-02KX02KX 02SrcMicrotubule/TubulinApoptosisU87 cellsGL261 cellsT98GInhibitorinhibitorinhibit

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