ChemicalBook > CAS DataBase List > CH5132799

CH5132799

Product Name
CH5132799
CAS No.
1007207-67-1
Chemical Name
CH5132799
Synonyms
CS-541;100843;PA-799;CS-1068;MEN-1611;CH5132799;CH-5033855;CH-5061565;CH-5089788;CH-5108135
CBNumber
CB02621133
Molecular Formula
C15H19N7O3S
Formula Weight
377.42
MOL File
1007207-67-1.mol
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CH5132799 Property

Boiling point:
751.1±70.0 °C(Predicted)
Density 
1.58
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Powder
pka
3.96±0.20(Predicted)
color 
White to gray
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

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.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

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

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
26410
Product name
CH5132799
Packaging
25mg
Price
$788
Updated
2024/03/01
Cayman Chemical
Product number
26410
Product name
CH5132799
Packaging
50mg
Price
$1082
Updated
2024/03/01
Cayman Chemical
Product number
26410
Product name
CH5132799
Packaging
5mg
Price
$198
Updated
2024/03/01
Cayman Chemical
Product number
26410
Product name
CH5132799
Packaging
10mg
Price
$355
Updated
2024/03/01
TRC
Product number
C291700
Product name
CH5132799
Packaging
5mg
Price
$220
Updated
2021/12/16
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CH5132799 Chemical Properties,Usage,Production

Uses

CH5132799 is a selective class I phosphoinositide 3-kinase (PI3K) inhibitor that targets human cancers harboring oncogenic PIK3CA mutations. CH5132799 also showed potent antiproliferative and antitumor activity.

Biological Activity

ch5132799 is an inhibitor of class i phosphatidylinositol 3-kinase (pi3k) with ic50 value of 14nm against pi3kα [1].ch5132799 shows inhibitory effect on class i pi3k with ic50 values of 0.014μm, 0.12μm, 0.5μm and 0.036μm against pi3kα, pi3kβ, pi3kδ and pi3kγ, respectively. pi3kα is especially sensitive to ch5132799. ch5132799 is a selective inhibitor. it shows less effect on class ii pi3ks, class iii pi3k and mtor. for other 26 protein kinases, ch5132799 nearly has no inhibition with ic50 value of > 10μm. ch5132799 is found to have potent antitumor activity. it exerts ic50 values of 0.2μm, 0.032μm, 0.056μm and 0.12μm in hct116, kpl-4, t-47d and sk-ov-3 cell lines, respectively. moreover, ch5132799 is oral available in animal models. treatment of ch5132799 shows strong tumor regression at dose of 12.5 mg/kg in mice bearing human breast cancer xenografts [1].

Synthesis

402960-38-7

1178564-27-6

1007207-67-1

GENERAL STEPS: To DMF (550 mL) under nitrogen protection were added 4-chloro-7-methanesulfonyl-2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine (57.9 g, 181.6 mmol), 2-amino-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine ( 48.2 g, 218.0 mmol), potassium phosphate (42.4 g, 199.8 mmol) and water (30 mL) and degassed. Subsequently, dichlorobis(triphenylphosphine)palladium(II) (1.3 g, 1.8 mmol) was added, degassed again, and then the reaction was stirred at 60 °C for 2 hours. After completion of the reaction, the reaction mixture was cooled in an ice bath, water (750 mL) was added and stirring was continued for 2 hours. The precipitate was collected by filtration and washed sequentially with water (240 mL) and acetone (240 mL) to give the crude product (75.6 g). The crude product (62.0 g) was suspended in water (1500 mL) and stirred at 50 °C for 1 hour. The suspension was filtered and washed sequentially with water (400 mL) and acetone (400 mL) to afford 5-(7-methylsulfonyl-2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine as an off-white solid (53.7 g, 96% yield).

in vivo

Mice bearing BT-474 tumors (n=14) are orally administered 50 mg/kg of Everolimus on a daily basis for 31 days and then randomized. After randomization, the mice are orally administered 50 mg/kg of Everolimus (n=4) and 12.5 mg/kg (n=5), and 25 mg/kg (n=5) of Izorlisib on a daily basis for 7 days. C, the vehicle-, Everolimus, and CH5132799-treated (25 mg/kg) tumors are resected at 4 hours after terminal administration in B, lysed, and analyzed by Western blotting. Izorlisib administration leads to a remarkable regression in a dose-dependent manner of the tumors regrown after the long-term Everolimus treatment. The tumors are resected at the end of treatment and analyzed by Western blotting with respect to PI3K pathway inhibition. Izorlisib suppresses various effectors in the PI3K pathway, including Akt, FoxO1, S6K, S6, and 4E-BP1, whereas Everolimus inhibits only phosphorylation of S6K and S6, both downstream effectors of mTORC1[1].

target

PI3Kα

IC 50

PI3Kα: 14 nM (IC50); PI3Kα-H1047R: 5.6 nM (IC50); PI3Kα-E545K: 6.7 nM (IC50); PI3Kα-E542K: 6.7 nM (IC50); PI3Kγ: 36 nM (IC50); PI3Kβ: 120 nM (IC50); PI3Kδ: 500 nM (IC50); PI3KC2β: 5.3 μM (IC50); mTOR: 1.6 μM (IC50)

References

[1] ohwada j, ebiike h, kawada h, et al. discovery and biological activity of a novel class i pi3k inhibitor, ch5132799. bioorganic & medicinal chemistry letters, 2011, 21(6): 1767-1772.

CH5132799 Preparation Products And Raw materials

Raw materials

Preparation Products

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CH5132799 Suppliers

China 116 India 2 United Kingdom 1 United States 19 Global 138
BOC Sciences
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1-631-485-4226; 16314854226
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United States
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MedChemexpress LLC
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021-58955995
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sales@medchemexpress.cn
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AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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Target molecule Corp.
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857-239-0968
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857-239-8801
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service1@targetmol.com
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Musechem
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+1-800-259-7612
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TargetMol Chemicals Inc.
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marketing@targetmol.com
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InvivoChem
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Cckinase, Inc.
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+1 (732)236-3202
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sales@cckinase.com
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Aladdin Scientific
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ApexBio Technology
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Cayman Chemical Company
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United States Biological
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1007207-67-1, CH5132799Related Search:

MK-2206 2HCl BAY 80-6946 (Copanlisib) Alpelisib (BYL719) Pictilisib PF-04691502 BEZ235 (NVP-BEZ235, Dactolisib)

  • CH5132799
  • CH5132799,5-(7-(Methylsulfonyl)-2-Morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyriMidin-4-yl)pyriMidin-2-aMine
  • [5-[7-Methylsulfonyl-2-(morpholin-4-yl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-yl]amine
  • 5-(7-(Methylsulfonyl)-2-Morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyriMidin-4-yl)pyriMidin-2-aMine
  • [5-[7-Methylsulfonyl-2-(morpholin-4-yl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-yl]amine CH5132799
  • CH5132799;CH 5132799;CH-5132799
  • 5-(7-(Methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-ami
  • CS-541
  • CS-1068
  • 100843
  • 5-(7-methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine
  • 2-Pyrimidinamine, 5-[6,7-dihydro-7-(methylsulfonyl)-2-(4-morpholinyl)-5H-pyrrolo[2,3-d]pyrimidin-4-yl]-
  • CH5132799 (PA-799)
  • CH5132799 USP/EP/BP
  • CH5132799 CH-5132799
  • CH5132799, 10 mM in DMSO
  • CH-5033855
  • CH-5061565
  • CH-5089788
  • CH-5108135
  • CH-5111436
  • CH-5138134
  • MEN-1611
  • PA-799
  • CH5132799 ，S2699
  • 1007207-67-1
  • Inhibitors
  • PI3K/Akt/mTOR
  • JAK
  • STAT
  • Akt
  • mTOR
  • PI3K