ChemicalBook > CAS DataBase List > LY3023414

LY3023414

Product Name: LY3023414
CAS No.: 1386874-06-1
Chemical Name: LY3023414
Synonyms: CS-2814;GTPL8918;LY3023414;LY-3023414;Samotolisib;LY3023414 (LY-3023414;Samotolisib (LY3023414;LY3023414(Samotolisib);Samotolisib, 10 mM in DMSO;Samotolisib (LY3023414) ，S8322
CBNumber: CB23048911
Molecular Formula: C23H26N4O3
Formula Weight: 406.48
MOL File: 1386874-06-1.mol

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LY3023414 Property

Boiling point:: 591.7±50.0 °C(Predicted)
Density: 1.239±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: ≥40.6 mg/mL in DMSO; insoluble in H2O; ≥28.9 mg/mL in EtOH
form: solid
pka: 13.65±0.29(Predicted)
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ApexBio Technology

Product number: B6099
Product name: LY3023414
Packaging: 25mg
Price: $345
Updated: 2021/12/16

ChemScene

Product number: CS-5361
Product name: Samotolisib
Purity: 99.77%
Packaging: 5mg
Price: $80
Updated: 2021/12/16

ApexBio Technology

Product number: B6099
Product name: LY3023414
Packaging: 5mg
Price: $105
Updated: 2021/12/16

Crysdot

Product number: CD31003664
Product name: LY3023414
Purity: 98+%
Packaging: 5mg
Price: $243
Updated: 2021/12/16

Crysdot

Product number: CD31003664
Product name: LY3023414
Purity: 98+%
Packaging: 10mg
Price: $347
Updated: 2021/12/16

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LY3023414 Chemical Properties,Usage,Production

Uses

Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations[1][2].

Biological Activity

ly3023414 is an atp competitive inhibitor of the class i pi3k isoforms, mtor and dna-pk.the phosphoinositide-3 kinase (pi3k)/akt/mammalian target of rapamycin (mtor) pathway is one of the most frequently altered pathways in cancer cell growth and survival.

in vitro

in biochemical testing against approximately 266 kinases, ly3023414 was found to potently and selectively inhibit class i pi3k isoforms, mtorc1/2, as well as dna-pk at low concentrations. in addition, inhibition of pi3k/akt/mtor signaling by ly3023414 led to g1 cell-cycle arrest and resulted in broad antiproliferative activity in cancer cell panel [1].

in vivo

ly3023414 showed high bioavailability and dose-dependent dephosphorylation of pi3k/akt/mtor pathway downstream substrates for 4 to 6 hours, indicating ly3023414's half-life of 2 hours. moreover, equivalent total daily doses of ly3023414 given either once or twice daily could inhibit tumor growth to the similar extents in multiple xenograft models, demonstrating intermittent target inhibition was sufficient for antitumor activity [1].

target

Target	Value
class I PI3K isoforms ()
mTOR kinase ()
DNA-PK ()

IC 50

64.9, 42.1, 10.6, and 19.1 nm for akt1(pt308), akt1 (ps473), p70s6(pt389), and s6rp(ps240/242), respectively.

References

[1] smith mc,mader mm,cook ja,et al. characterization of ly3023414, a novel pi3k/mtor dual inhibitor eliciting transient target modulation to impede tumor growth. mol cancer ther.2016 oct;15(10):2344-2356.

LY3023414 Preparation Products And Raw materials

Raw materials

Preparation Products

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1386874-06-1, LY3023414Related Search:

LY 294002 Hydrochloride LY2157299 LY-3177833 2-(4-((4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)oxy)pyridin-2-yl)amino)pyridin-2-yl)propan-2-ol LY3214996 LY2409881 Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2 LY2955303 LY 334370 HYDROCHLORIDE

LY3023414

LY-3023414

8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one

LY3023414(Samotolisib)

LY3023414;LY-3023414;LY 3023414

CS-2814

GTPL8918

2H-Imidazo[4,5-c]quinolin-2-one, 1,3-dihydro-8-[5-(1-hydroxy-1-methylethyl)-3-pyridinyl]-1-[(2S)-2-methoxypropyl]-3-methyl-

Samotolisib

Samotolisib (LY3023414

(S)-8-(5-(2-Hydroxypropan-2-yl)pyridin-3-yl)-1-(2-methoxypropyl)-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one

Inhibitor,mTOR,LY-3023414,Phosphoinositide 3-kinase,DNA-dependent protein kinase,inhibit,Autophagy,LY 3023414,Samotolisib,DNA-PK,PI3K,Mammalian target of Rapamycin

Samotolisib, 10 mM in DMSO

Samotolisib (LY3023414) ，S8322

LY3023414 (LY-3023414

1386874-06-1