[CAS NO. 897016-82-9] KX2-391 (Tirbanibulin)
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PRODUCTS SPECIFICATIONS [897016-82-9]
Store
Catalog
SLK-S2700
Brand
Selleck
CAS
897016-82-9
DESCRIPTION [897016-82-9]
Overview
| MDL | MFCD18633218 |
|---|---|
| Molecular Weight | 431.53 |
| Molecular Formula | C26H29N3O3 |
| SMILES | O=C(NCC1=CC=CC=C1)CC2=NC=C(C3=CC=C(OCCN4CCOCC4)C=C3)C=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3173 mL | 11.5867 mL | 23.1734 mL |
| 5 mM | 0.4635 mL | 2.3173 mL | 4.6347 mL |
| 10 mM | 0.2317 mL | 1.1587 mL | 2.3173 mL |
| 50 mM | 0.0463 mL | 0.2317 mL | 0.4635 mL |
Description
KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with of 9-60 nM in cancer cell lines. Phase 2.
Targets
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. 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.
In vivo
In pre-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis.
References
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