KX2-391
Cat. No.: DC8023
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Chemical Structure
897016-82-9
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Field of application
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.
Cas No.: |
897016-82-9 |
Chemical Name: |
Tirbanibulin |
Synonyms: |
KX 01;KX2-391;N-benzyl-2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]acetamide;KX-01;Tirbanibulin;N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide;4V9848RS5G;2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]-~{N}-(phenylmethyl)ethanamide;KX2391;Tirbanibulin [USAN];MLS006011272;KX01;GTPL7957;HUNGUWOZPQBXGX-UHFFFAOYSA-N;HMS3656J15;BCP02845;WHO 10864;s2700;BDBM50303801;N-benzyl-2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]aceta;5-[4-[2-(4-Morpholinyl)ethoxy]phenyl]-N-(phenylmethyl)-2-pyridineacetamide (ACI);Klisyri;KX 2-391;KX 2-931;KX O1 |
SMILES: |
O=C(CC1C=CC(C2C=CC(OCCN3CCOCC3)=CC=2)=CN=1)NCC1C=CC=CC=1 |
Formula: |
C26H29N3O3 |
M.Wt: |
431.52676653862 |
Sotrage: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: |
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. |
In Vivo: |
Orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer[2]. |
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 (GI50=9 nM), PLC/PRF/5 (GI50=13 nM), Hep3B (GI50=26 nM), and HepG2 (GI50=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]. |
MSDS
COA
LOT NO. |
DOWNLOAD |
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2018-0101 |
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2018-0101 |
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