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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 structure

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: MLN0128;INK-128;TAK-228;MLN0218;MLNO128;INK-0128;INK128, >=98%;INK 128; INK128;INK 128 (MLN0128);Sapanisertib (NK128

CBNumber:: CB92553620

Molecular Formula:: C15H15N7O

Molecular Weight:: 309.33

MDL Number:: MFCD22124893

MOL File:: 1224844-38-5.mol

Last updated:2023-05-18 11:31:20

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

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.
FDA UNII	JGH0DF1U03

5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine price More Price(45)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Cayman Chemical	11811	INK128 ≥98%	1224844-38-5	1mg	$31	2024-03-01	Buy
Cayman Chemical	11811	INK128 ≥98%	1224844-38-5	5mg	$61	2024-03-01	Buy
Cayman Chemical	11811	INK128 ≥98%	1224844-38-5	10mg	$105	2024-03-01	Buy
Cayman Chemical	11811	INK128 ≥98%	1224844-38-5	50mg	$220	2024-03-01	Buy
TRC	A602050	3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine	1224844-38-5	10mg	$90	2021-12-16	Buy

Product number	Packaging	Price	Buy
11811	1mg	$31	Buy
11811	5mg	$61	Buy
11811	10mg	$105	Buy
11811	50mg	$220	Buy
A602050	10mg	$90	Buy

5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine Chemical Properties,Uses,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) Hsieh?et al.?(2012),?The translational landscape of mTOR signaling steers cancer initiation and metastasis; Nature,?485?55 2) Gokmen-Polar?et al.?(2012)?Investigational drug MLN0128, a novel TORC1/2 inhibitor, demonstrates potent oral antitumor activity in human breast cancer xenograft models; Breast Cancer Res. Treat.,?136?673

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

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

Global( 164)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49390	58
SHANGHAI T&W PHARMACEUTICAL CO., LTD.	+86-021-61551413 +8618813727289	contact@trustwe.com	China	5738	58
Tianjin Xinshengjiahe Science & Technology Development Co,.Ltd	+86-86-22-87899925 +86-8618522618860	18522618860@163.com	China	694	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6313	58

Supplier	Advantage
ATK CHEMICAL COMPANY LIMITED	60
career henan chemical co	58
Hubei Jusheng Technology Co.,Ltd.	58
BOC Sciences	58
Chongqing Chemdad Co., Ltd	58
CONIER CHEM AND PHARMA LIMITED	58
SHANGHAI T&W PHARMACEUTICAL CO., LTD.	58
Tianjin Xinshengjiahe Science & Technology Development Co,.Ltd	58
TargetMol Chemicals Inc.	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	58

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

Image	Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
	2021-10-08	Sapanisertib;MLN0218 1224844-38-5	US $0.00-0.00 / g	1g	98%	100kgs	Wuhan Nutra Biotechnology Co.,Ltd
	2019-07-06	5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine 1224844-38-5	US $2.00 / kg	1kg	99%	100kg	Career Henan Chemical Co

Sapanisertib;MLN0218
1224844-38-5
US $0.00-0.00 / g
98%
Wuhan Nutra Biotechnology Co.,Ltd

5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine
1224844-38-5
US $2.00 / kg
99%
Career Henan Chemical Co

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

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

1224844-38-5(5-(4-aMino-1-isopropyl-1H-pyrazolo[3,4-d]pyriMidin-3-yl)benzo[d]oxazol-2-aMine)Related 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 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) 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) 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 1224844-38-5 C15H15N7O Inhibitors PI3K/Akt/mTOR Akt mTOR PI3K