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

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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:

CYCLOPAMINE Adapalene AG 490 Brefeldin A Amino alcohol 2,6-Dichlorobenzoxazole Thianaphthene 2-(P-TOLYL)BENZOXAZOLE Quinazoline 2-Phenylbenzoxazole Everolimus Bortezomib AZD-8055 MK-2206 2HCl Rapamycin AZD2014 Fluensulfone JNJ 16259685

  • 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