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PI3K inhibitor

Product Name
PI3K inhibitor
CAS No.
1202884-94-3
Chemical Name
PI3K inhibitor
Synonyms
CAY10626;PI3K-IN-22;Antitumor Drug;PI3K inhibitor;CAY10626, PI3Kalpha/mTOR inhibitor;N-[2-(dimethylamino)ethyl]-N-methyl-4-[({4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]phenyl}carbamoyl)amino]benzamide;BenzaMide, N-[2-(diMethylaMino)ethyl]-N-Methyl-4-[[[[4-[4-(4-Morpholinyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyriMidin-2-yl]phenyl]aMino]carbonyl]aMino]-
CBNumber
CB62487667
Molecular Formula
C31H35F3N8O3
Formula Weight
624.66
MOL File
1202884-94-3.mol
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PI3K inhibitor Property

Density 
1.35±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 15 mg/ml; DMSO: 15 mg/ml; DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
form 
A crystalline solid
pka
13.74±0.70(Predicted)
color 
White to light yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
13838
Product name
CAY10626
Purity
≥98%
Packaging
1mg
Price
$105
Updated
2024/03/01
Cayman Chemical
Product number
13838
Product name
CAY10626
Purity
≥98%
Packaging
5mg
Price
$459
Updated
2024/03/01
Cayman Chemical
Product number
13838
Product name
CAY10626
Purity
≥98%
Packaging
10mg
Price
$816
Updated
2024/03/01
Cayman Chemical
Product number
13838
Product name
CAY10626
Purity
≥98%
Packaging
25mg
Price
$1783
Updated
2024/03/01
TRC
Product number
C227025
Product name
CAY10626
Packaging
2.5mg
Price
$295
Updated
2021/12/16
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PI3K inhibitor Chemical Properties,Usage,Production

Description

The PI3Kinases are important downstream effectors of KRAS signaling. In preclinical studies, buparlisib (BKM120), a PI3K inhibitor, when combined with MEK inhibitor (PD1056309) led to significant synergistic activity in KRAS mutant NSCLC cell lines.

Uses

PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer[1].

Definition

ChEBI: CAY10626 is a member of ureas.

in vivo

PI3K-IN-22 (25 mg/kg; i.v.) suppresses phosphorylation of Akt T308, Akt S473 and S6K in MDA361 breast tumor cells up to 8 h in MDA361 tumor bearing nude mice demonstrated by biomarker studies[1].
PI3K-IN-22 (50, 25, 10 mg/kg; i.v.; once daily for 5 days weekly; 2 rounds) shows good antitumor efficacy in MDA361 tumor xenograft nude mice model[1].
PI3K-IN-22 (25 mg/kg; i.v.; a single dose) has a blood concentrationsat value of 1731 ng/mL at 8 h[1].

Animal Model:MDA361 tumor xenograft nude mice model[1]
Dosage:50, 25, 10 mg/kg
Administration:i.v., once daily for 5 days weekly (2 rounds)
Result:Exhibited significant tumor regression in 50 mg/kg and no tumor regrowth until day 32.
Exhibited tumor growth inhibition in 25 and 10 mg/kg.

IC 50

PI3Kα: 0.9 nM (IC50); mTOR: 0.6 nM (IC50)

References

[1] Chen Z, et al. Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors. J Med Chem. 2010 Apr 22;53(8):3169-82. DOI:10.1021/jm901783v

PI3K inhibitor Preparation Products And Raw materials

Raw materials

Preparation Products

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PI3K inhibitor Suppliers

Canada 1 China 27 India 1 United States 7 Global 36
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
Advantage
65
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32467
Advantage
58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
ProdList
11218
Advantage
58
Shanghai Zeye Biotechnology Co., Ltd.
Tel
021-57896695 13122364865
Email
sale1@shzysw.net
Country
China
ProdList
9779
Advantage
58
Energy Chemical
Tel
021-58432009 400-005-6266
Fax
021-58436166
Email
marketing@energy-chemical.com
Country
China
ProdList
44918
Advantage
58
TargetMol Chemicals Inc.
Tel
4008200310
Email
marketing@tsbiochem.com
Country
China
ProdList
24960
Advantage
58
Shanghai Yifei Biotechnology Co. , Ltd.
Tel
021-65675885 18964387627
Email
customer_service@efebio.com
Country
China
ProdList
11972
Advantage
58
Cayman Chemical Company
Tel
800-364-9897
Email
sales@caymanchem.com
Country
China
ProdList
6838
Advantage
58

1202884-94-3, PI3K inhibitorRelated Search:


  • PI3K inhibitor
  • Antitumor Drug
  • CAY10626
  • BenzaMide, N-[2-(diMethylaMino)ethyl]-N-Methyl-4-[[[[4-[4-(4-Morpholinyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyriMidin-2-yl]phenyl]aMino]carbonyl]aMino]-
  • N-[2-(dimethylamino)ethyl]-N-methyl-4-[({4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]phenyl}carbamoyl)amino]benzamide
  • PI3K-IN-22
  • CAY10626, PI3Kalpha/mTOR inhibitor
  • 1202884-94-3
  • C31H35F3N8O3