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1224844-38-5

1224844-38-5 structure

1224844-38-5 structure

Name: Sapanisertib (MLN0128)
Chemical Name: 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine
CAS Number: 1224844-38-5
Molecular Formula: C₁₅H₁₅N₇O
Molecular Weight: 309.326
Catalog: Biochemical Inhibitor PI3K/Akt/mTOR inhibitor (PI3K/Akt/mTOR) mTOR inhibitor
Create Date: 2018-06-02 08:00:00
Modify Date: 2026-07-01 16:46:10
Sapanisertib (INK-128) is a ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.

Name	5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine
Synonyms	5-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine INK 128 (MLN0128) CB-228 TAK-228 INK-0128 Sapanisertib INK-128 MLN0128 MLNO128 Sapanisertib a potent and selective mTOR inhibitor 3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine Sapanisertib (NK128 Sapanisertib (Synonyms: INK-128) ，min UNII-JGH0DF1U03 3-(2-Amino-1,3-benzoxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine Sapanisertib, 10 mM in DMSO INK-128(Sapanisertib) 3-(2-Ami-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 3-(2-amino-5-benzoxazolyl)-1-(1-methylethyl) ink-128/ink128 MLN0218 ink 128 INK 128; INK128 cs-0557 INK 128 (MLN0128);INK-128;MLN0128 INK128, >= Sapanisertib TAK-228 INK-128 MLN0128 TAK228 INK128 MLN-0128 Sapanisertib (INK-128) UNII:JGH0DF1U03 5-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine //BP (4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine INK-128 3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 5-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-amine(INK-128)

Description	Sapanisertib (INK-128) is a ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> PI3K/Akt/mTOR >> mTOR Research Areas >> Cancer
Target	mTOR:1 nM (IC50) mTORC1 mTORC2 PI3Kα:219 nM (IC50) PI3Kβ:5.293 μM (IC50) PI3Kδ:230 nM (IC50) PI3Kγ:221 nM (IC50) Autophagy
In Vitro	Sapanisertib (INK-128) exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases[1]. Sapanisertib (INK-128) selectively decreases the expression of YB1, MTA1, vimentin and CD44 at the protein but not transcript level in PC3 cells. Sapanisertib (INK-128) decreases the invasive potential of PC3 prostate cancer cells. Furthermore, Sapanisertib (INK-128) inhibits cancer cell migration starting at 6 h of treatment, precisely correlating with when decreases in the expression of pro-invasion genes are evident, but preceding any changes in the cell cycle or overall global protein synthesis[2].
In Vivo	In a ZR-75-1 breast cancer xenograft model, Sapanisertib (INK-128) shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day[1]. 4EBP1 and p70S6K1/2 phosphorylation is completely restored to wild-type levels after treatment with INK128 in PtenL/L mice. Sapanisertib (INK-128) treatment results in a 50% decrease in prostatic intraepithelial neoplasia (PIN) lesions in PtenL/L mice and induces programmed cell death in multiple cancer cell lines in mice[2].
Cell Assay	PC3 cells are treated with the appropriate drug for 48 h, and proliferation is measured using CellTiter-Glo Luminescent reagent. The concentration of Sapanisertib (INK-128) necessary to achieve inhibition of cell growth by 50% (IC50) is calculated using concentrations ranging from 20.0 μM to 0.1 nM (12-point curve).
Animal Admin	Nude mice are inoculated subcutaneously in the right subscapular region with 5×106 MDA-MB-361 cells. After tumours reach a size of 150-200 mm3, mice are randomLy assigned into vehicle control or treatment groups. Sapanisertib (INK-128) is formulated in 5% polyvinylpropyline, 15% NMP, 80% water and administered by oral gavage at 0.3 mg/kg and 1 mg/kg daily.
References	[1]. Liu A, et al. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55. [2]. Hsieh AC, et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22;485(7396):55-61.

Density	1.6±0.1 g/cm3
Boiling Point	598.8±60.0 °C at 760 mmHg
Molecular Formula	C₁₅H₁₅N₇O
Molecular Weight	309.326
Flash Point	315.9±32.9 °C
Exact Mass	309.133820
PSA	121.67000
LogP	1.95
Vapour Pressure	0.0±1.7 mmHg at 25°C
Index of Refraction	1.829
Storage condition	-20°C

83255-86-1 structure

83255-86-1

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1224844-38-5 structure

1224844-38-5

Literature: WO2013/23184 A1, ; WO 2013/023184 A1

40925-68-6 structure

40925-68-6

~%

1224844-38-5 structure

1224844-38-5

Literature: WO2013/23184 A1, ; WO 2013/023184 A1

64037-07-6 structure

64037-07-6

~%

1224844-38-5 structure

1224844-38-5

Literature: WO2013/23184 A1, ; WO 2013/023184 A1

Precursor 3
83255-86-1 40925-68-6 64037-07-6
DownStream 0

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