DS-1205b free base - ≥99% , CAS No.1855860-24-0

CAS: 1855860-24-0 Cat. No.: D648321 Molecular Weight: 735.80 PubChem CID: 129110632

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

DS-1205b free base is a potent and selective inhibitor of AXL kinase , with an IC 50 of 1.3 nM. DS-1205b free base also inhibits MER , MET , and TRKA , with IC 50 s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo

In Vitro

DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC 50 =2.7 nM). DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI 50 >10,000 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: NIH3T3-AXL cells Concentration: 1, 10, 100, 1000, 10000 μM Incubation Time: 2, 24 hours Result: Completely inhibited the phosphorylation of AXL at concentrations above 10 nM. Slightly inhibited the phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.

In Vivo

DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks 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.

Form:Solid

IC50& Target:AXL 1.3 nM (IC 50 ) MER 63 nM (IC 50 ) TrkA 407 nM (IC 50 ) Met 104 nM (IC 50 )

Specifications

Specifications & Purity

≥99%

Biochemical and Physiological Mechanisms

DS-1205b free base is a potent and selective inhibitor of AXL kinase , with an IC 50 of 1.3 nM. DS-1205b free base also inhibits MER , MET , and TRKA , with IC 50 s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vit

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥99%

Names and Identifiers

• Canonical Smiles: CC1=CN=C(C=C1)C2=CN(C=C(C2=O)C(=O)NC3=CC(=C(C=C3)C4=C(N=CC(=C4)C5=CC(=C(C=C5)OCC6COCCO6)OC)N)F)CC7CCOCC7
• IUPAC Name: N-[4-[2-amino-5-[4-[[(2R)-1,4-dioxan-2-yl]methoxy]-3-methoxyphenyl]pyridin-3-yl]-3-fluorophenyl]-5-(5-methylpyridin-2-yl)-1-(oxan-4-ylmethyl)-4-oxopyridine-3-carboxamide
• InChIKey: ZOEILZXFYPPMTR-SSEXGKCCSA-N
• INCHI: 1S/C41H42FN5O7/c1-25-3-7-36(44-18-25)33-21-47(20-26-9-11-51-12-10-26)22-34(39(33)48)41(49)46-29-5-6-31(35(42)17-29)32-15-28(19-45-40(32)43)27-4-8-37(38(16-27)50-2)54-24-30-23-52-13-14-53-30/h3-8,15-19,21-22,26,30H,9-14,20,23-24H2,1-2H3,(H2,43,45)(H,46,49)/t30-/m1/s1
• PubChem CID: 129110632
• Molecular Weight: 735.80

Chemical and Physical Properties

• Solubility: DMSO : 50 mg/mL (67.95 mM; Need ultrasonic)