[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]-

Product 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 No.: 1855860-24-0
Chemical 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]-
Synonyms: AB-329;DS-1205;DS-1206;DS-1206b;DS-1205b;DS-1205b free base;DS-1205, 10 mM in DMSO;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;N-{4-[2-amino-5-(4-{[(2R)-1,4-dioxan-2-yl]methoxy}-3-methoxyphenyl)pyridin-3-yl]-3-fluorophenyl}-5-methyl-1'-[(oxan-4-yl)methyl]-4'-oxo-1',4'-dihydro-[2,3'-bipyridine]-5'-carboxamide;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]-
CBNumber: CB98138108
Molecular Formula: C41H42FN5O7
Formula Weight: 735.8
MOL File: 1855860-24-0.mol

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[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]- Property

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)
pka: 10.74±0.70(Predicted)
form: Solid
color: Off-white to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0115020
Product name: DS-1205b(freebase)
Purity: 99.92%
Packaging: 5mg
Price: $550
Updated: 2021/12/16

ChemScene

Product number: CS-0115020
Product name: DS-1205b(freebase)
Purity: 99.92%
Packaging: 10mg
Price: $950
Updated: 2021/12/16

ChemScene

Product number: CS-0115020
Product name: DS-1205b(freebase)
Purity: 99.92%
Packaging: 25mg
Price: $1950
Updated: 2021/12/16

ChemScene

Product number: CS-0115020
Product name: DS-1205b(freebase)
Purity: 99.92%
Packaging: 50mg
Price: $3250
Updated: 2021/12/16

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[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]- Chemical Properties,Usage,Production

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

[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]- Preparation Products And Raw materials

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Preparation Products

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[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]- Suppliers

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1855860-24-0, [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]-Related Search:

[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]-

DS-1206b

DS-1206

DS-1205

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]-

N-{4-[2-amino-5-(4-{[(2R)-1,4-dioxan-2-yl]methoxy}-3-methoxyphenyl)pyridin-3-yl]-3-fluorophenyl}-5-methyl-1'-[(oxan-4-yl)methyl]-4'-oxo-1',4'-dihydro-[2,3'-bipyridine]-5'-carboxamide

DS-1205, 10 mM in DMSO

AB-329

DS-1205b

1855860-24-0

C41H42FN5O7