| Identification | Back Directory | [Name]
[2,3'-Bipyridine]-5'-carboxamide, N-[4-[2-amino-5-[4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-methoxyphenyl]-3-pyridinyl]-3-fluorophenyl]-1',4'-dihydro-5-methyl-4'-oxo-1'-[(tetrahydro-2H-pyran-4-yl)methyl]- | [CAS]
1855860-24-0 | [Synonyms]
DS-1206
DS-1205
DS-1206b
DS-1205b free base
TRKA,c-Met/HGFR,migration,Axl,Tyro3,Trk Receptor,MET,DS 1205,Mer,Tropomyosin related kinase receptor,tumor,DS1205,kinase,inhibit,Inhibitor,DS-1205b,TAM Receptor,NIH3T3
[2,3'-Bipyridine]-5'-carboxamide, N-[4-[2-amino-5-[4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-methoxyphenyl]-3-pyridinyl]-3-fluorophenyl]-1',4'-dihydro-5-methyl-4'-oxo-1'-[(tetrahydro-2H-pyran-4-yl)methyl]- | [Molecular Formula]
C41H42FN5O7 | [MDL Number]
MFCD33029318 | [MOL File]
1855860-24-0.mol | [Molecular Weight]
735.8 |
| Chemical Properties | Back Directory | [Boiling point ]
889.4±65.0 °C(Predicted) | [density ]
1.307±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (67.95 mM; Need ultrasonic) | [form ]
Solid | [pka]
10.74±0.70(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Uses]
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo[1]. | [in vivo]
DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice[1]. | Animal Model: | Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks[1] | | Dosage: | 3.1, 6.3, 13, 25, 50 mg/kg | | Administration: | P.o. twice daily for 5 days | | Result: | Inhibited tumor growth by 39-94%.
Reduced the phosphorylation of both AXL and AKT in tumors. |
| [IC 50]
Axl; Mer; AXL: 1.3 nM (IC50); MER: 63 nM (IC50); TrkA: 407 nM (IC50); Met: 104 nM (IC50) | [References]
[1] Jimbo T, et, al. DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model. Oncotarget. 2019 Aug 27;10(50):5152-5167. DOI:10.18632/oncotarget.27114 |
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| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 +86-19945035818 |
| Website: |
http://www.topule.com/ |
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