ChemicalBook > CAS DataBase List > 5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine

5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine

Product Name: 5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine
CAS No.: 1224844-38-5
Chemical Name: 5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine
Synonyms: CB-228;MLN0128;INK-128;TAK-228;MLN0218;MLNO128;INK-0128;INK128, >=98%;INK 128; INK128;INK 128 (MLN0128)
CBNumber: CB92553620
Molecular Formula: C15H15N7O
Formula Weight: 309.33
MOL File: 1224844-38-5.mol

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5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine Property

Melting point:: 270-272°C (dec.)
Boiling point:: 598.8±60.0 °C(Predicted)
Density: 1.64
storage temp.: -20°C
solubility: Soluble in DMSO (up to 25 mg/ml)
pka: 3.77±0.30(Predicted)
form: solid
color: Off-white
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChI: InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)
InChIKey: GYLDXIAOMVERTK-UHFFFAOYSA-N
SMILES: C1=NC(N)=C2C(C3=CC=C4OC(N)=NC4=C3)=NN(C(C)C)C2=N1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H303May be harmfulif swallowed

H320Causes eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

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

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 11811
Product name: INK128
Purity: ≥98%
Packaging: 1mg
Price: $31
Updated: 2024/03/01

Cayman Chemical

Product number: 11811
Product name: INK128
Purity: ≥98%
Packaging: 5mg
Price: $61
Updated: 2024/03/01

Cayman Chemical

Product number: 11811
Product name: INK128
Purity: ≥98%
Packaging: 10mg
Price: $105
Updated: 2024/03/01

Cayman Chemical

Product number: 11811
Product name: INK128
Purity: ≥98%
Packaging: 50mg
Price: $220
Updated: 2024/03/01

TRC

Product number: A602050
Product name: 3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Packaging: 10mg
Price: $90
Updated: 2021/12/16

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5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine Chemical Properties,Usage,Production

Description

INK128 is an inhibitor of TORC1/2, acting as an ATP-dependent inhibitor of mTOR kinase (IC₅₀ = 1 nM). It blocks the phosphorylation of downstream substrates of both TORC1 and TORC2. INK128 interferes with the growth of cell lines which are resistant to rapamycin and pan-PI3K inhibitors. Moreover, daily, oral administration of INK128 inhibits angiogenesis and tumor growth in several xenograft models. The effects of INK128 on gene expression also reduce invasion and metastasis.

Uses

3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine is a potent and selective TORC1/2 inhibitor with broad oral antitumor activity. TORC1/2 inhibitors are mechanistically distinct from rapamycinand offer a compelling approach to the treatment of cancer by targeting translational control, cell metabolism, growth andangiogenesis.

Definition

ChEBI: 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine is a benzoxazole.

Biological Activity

Sapanisertib (MLN0128, INK 128, TAK-228) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.

in vitro

INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors.

in vivo

In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models.

target

mTOR

References

[1] ANDREW C. HSIEH. The translational landscape of mTOR signalling steers cancer initiation and metastasis[J]. Nature, 2012, 485 7396: 55-61. DOI:10.1038/nature10912
[2] YESIM GÖKMEN-POLAR. Investigational drug MLN0128, a novel TORC1/2 inhibitor, demonstrates potent oral antitumor activity in human breast cancer xenograft models.[J]. Breast Cancer Research and Treatment, 2012, 136 3: 673-682. DOI:10.1007/s10549-012-2298-8

5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from 5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine manufacturers

Wuhan Nutra Biotechnology Co.,Ltd

Product: Sapanisertib;MLN0218 1224844-38-5
Price: US $0.00-0.00/g
Min. Order: 1g
Purity: 98%
Supply Ability: 100kgs
Release date: 2021-05-24

Career Henan Chemical Co

Product: 5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine 1224844-38-5
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-24

1224844-38-5, 5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMineRelated Search:

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5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine

3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

INK-128

3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine

INK-128 3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

MLN0128

5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine

-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine

INK 128 (MLN0128)

INK128, >=98%

INK-128(Sapanisertib)

INK-0128

INK 128 (MLN0128),95+

INK 128 (MLN0128);INK-128;MLN0128

5-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-amine(INK-128)

Sapanisertib (INK-128)

Sapanisertib, 98%, a potent and selective mTOR inhibitor

Sapanisertib (INK 128, MLN0128)

INK 128; INK128

Sapanisertib (INK 128, MLN0128,TAK-228)

TAK-228

1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 3-(2-amino-5-benzoxazolyl)-1-(1-methylethyl)-

5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine USP/EP/BP

MLN0218

Sapanisertib (NK128

Sapanisertib (MLN0128)

MLNO128

Sapanisertib TAK-228 INK-128 MLN0128 TAK228 INK128

3-(2-Ami-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Sapanisertib, 10 mM in DMSO

CB-228

Sapanisertib (Synonyms: INK-128) ，98%min

1224844-38-5

C15H15N7O

Inhibitors

PI3K/Akt/mTOR

Akt

mTOR

PI3K