ChemicalBook > CAS DataBase List > OSI-027

OSI-027

Product Name
OSI-027
CAS No.
936890-98-1
Chemical Name
OSI-027
Synonyms
CS-436;OSI-027;ASP4786;CPD2801;OSI-027, >=98%;OSI027;OSI 027;OSI-027 USP/EP/BP;OSI-027, 10 mM in DMSO;OSI-027;OSI 027;ASP4786;trans-4-[4-Amino-5-(7-methoxy-1H-i
CBNumber
CB42538725
Molecular Formula
C21H22N6O3
Formula Weight
406.44
MOL File
936890-98-1.mol
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OSI-027 Property

Melting point:
>149°C (subl.)
Density 
1.59
storage temp. 
Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility 
DMSO (Slightly)
pka
4.44±0.10(Predicted)
form 
Solid
color 
Pale Beige to Light Beige
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
17379
Product name
OSI-027
Purity
≥98%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
17379
Product name
OSI-027
Purity
≥98%
Packaging
5mg
Price
$134
Updated
2024/03/01
Cayman Chemical
Product number
17379
Product name
OSI-027
Purity
≥98%
Packaging
10mg
Price
$249
Updated
2024/03/01
Cayman Chemical
Product number
17379
Product name
OSI-027
Purity
≥98%
Packaging
50mg
Price
$670
Updated
2024/03/01
TRC
Product number
A611910
Product name
4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]Triazin-7-yl)cyclohexanecarboxylicAcid
Packaging
1mg
Price
$65
Updated
2021/12/16
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OSI-027 Chemical Properties,Usage,Production

Description

The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin ) and regulate different pathways. OSI-027 is an inhibitor of the catalytic site of mTOR and, as a result, inhibits both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively). It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase. OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 μM. OSI-027 is effective in vivo, blocking the phosphorylation of targets of mTORC1 and mTORC2 and suppressing tumor growth in several different human xenograft models.

Uses

OSI-027 is a kinase inhibitor with anti-tumor activity, used in treatment of breast cancer.

Definition

ChEBI: 4-[4-amino-5-(7-methoxy-2-indolylidene)-1H-imidazo[5,1-f][1,2,4]triazin-7-yl]-1-cyclohexanecarboxylic acid is a member of indoles.

in vivo

Effects on GEO colorectal xenograft growth treated with Rapamycin or OSI-027 for 12 days are consistent with our in vitro experiments. Treatment with Rapamycin (20 mg/kg) inhibits phospho-S6 and phospho-4E-BP1, while Akt phosphorylation is increased by 29%. In contrast, OSI-027 (65 mg/kg) inhibits both mTORC1 and mTORC2 effectors. After 2 hours, decreased 4E-BP1, Akt, and S6 phosphorylation is observed and inhibition of S6 and Akt is sustained for 24 hours. The plasma drug concentration of OSI-027 inversely correlated with these effects on mTORC1 and mTORC2 signaling. The median plasma drug concentration with OSI-027 is 21.3 μM at 2 hours and 14.9 μM at 8 hours. The in vivo efficacy of OSI-027 plus Sunitinib is tested in H292 human lung and Ovcar-5 human ovarian xenograft tumors. H292 tumors, treated with OSI-027 (50 mg/kg) for 21 days have 61% median tumor growth inhibition for the duration of treatment (TGI). Sunitinib (40 mg/kg) for 21 days had 47% median TGI. Combining OSI-027 with Sunitinib, however, has a median TGI of 100% with 59% maximal tumor regression, a statistically significant improvement over either agent alone. Ovcar-5 xenograft tumors treated with OSI-027 or Sunitinib have a 55% and 68% median TGI, respectively. OSI-027 administered with Sunitinib has a significantly better median TGI of 100% with 38% maximal tumor regression[1].
In the Rapamycin (RAPA) group, three rats exhibit symptoms typical of LTx-aGVHD and die 27 to 35 days after liver transplantation (LT); the remaining five rats do not develop LTx-aGVHD symptoms and survive for more than 100 days. In contrast, seven rats in the OSI-027 group survive for more than 100 days without symptoms of LTx-aGVHD, and only one rat exhibits LTx-aGVHD symptoms and dies on day 33 after LT[3].

target

mTORC

IC 50

mTOR: 4 nM (IC50); mTORC1: 22 nM (IC50); mTORC2: 65 nM (IC50); PI3K-γ: 0.42 μM (IC50); PI3K-α: 1.3 μM (IC50); DNA-PK: 1 μM (IC50); Autophagy

References

[1] bhagwat s v, gokhale p c, crew a p, et al. preclinical characterization of osi-027, a potent and selective inhibitor of mtorc1 and mtorc2: distinct from rapamycin. molecular cancer therapeutics, 2011, 10(8): 1394-1406.

OSI-027 Preparation Products And Raw materials

Raw materials

Preparation Products

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OSI-027 Suppliers

Canada 1 China 119 India 1 United States 19 Global 140
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
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China
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2922
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J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
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76
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
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61
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
ProdList
1856
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NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
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Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
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61
UHN Shanghai Research & Development Co., Ltd.
Tel
021-58958002 18930822973
Fax
+86 (21) 5895-8628
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sales@uhnshanghai.com
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China
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998
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Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-6206333 13167063860
Fax
021-50323701
Email
anhua.mao@aladdin-e.com
Country
China
ProdList
25003
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65
shanghai cooperpharm co.,LTD .
Tel
+86-021-58975553
Fax
+86-021-58975554
Email
sales@cooperpharm.com
Country
China
ProdList
1210
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56
Bsisun HK Imoprt And Export Company Limited
Tel
+86-18068513926
Fax
0086-519-85153711
Country
China
ProdList
1277
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View Lastest Price from OSI-027 manufacturers

Career Henan Chemical Co
Product
OSI-027 936890-98-1
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
ask
Release date
2018-12-23

936890-98-1, OSI-027Related Search:

LY 294002 Hydrochloride 3'-Amino-4'-methoxyacetanilide p-Anisidine-3-sulfonic acid trans-4-Aminocyclohexanol AZD-8055 VE 822 Ibrutinib Rapamycin BEZ235 (NVP-BEZ235, Dactolisib)

  • OSI-027
  • trans-4-[4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexanecarboxylic acid
  • 4-(4-aMino-5-(7-Methoxy-1H-indol-2-yl)-1,2-dihydroiMidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid hydrochloride
  • 4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f] [1,2,4]Triazin-7-yl)cyclohexanecarboxylic Acid
  • (1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[1,5-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid
  • ASP4786
  • OSI-027 trans-4-[4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexanecarboxylic acid
  • trans-4-[4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexanecarboxylic acid OSI-027
  • OSI-027, >=98%
  • CYCLOHEXANECARBOXYLIC ACID, 4-[4-AMINO-5-(7-METHOXY-1H-INDOL-2-YL)IMIDAZO[5,1-F][1,2,4]TRIAZIN-7-YL]-, TRANS-
  • trans-4-[4-Amino-5-(7-methoxy-1H-i
  • (1r,4r)-4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo-[5,1-f][1,2,4]triazin-7-yl)cyclohexaneca
  • OSI-027;OSI 027;ASP4786
  • CS-436
  • CPD2801
  • OSI027;OSI 027
  • OSI-027 USP/EP/BP
  • OSI-027 (ASP-4786, CERC-006, AEVI-006)
  • OSI-027, 10 mM in DMSO
  • 936890-98-1
  • Akt
  • mTOR
  • PI3K
  • Inhibitors