ChemicalBook > CAS DataBase List > 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine

5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine

Product Name
5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine
CAS No.
1225037-39-7
Chemical Name
5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine
Synonyms
PQR309;CS-2024;PI3K-IN-2;Bimiralisib;PQR-309, >98%;PQR309 Bimiralisib;Bimiralisib (PQR309);PQR309;PQR 309;PQR-309;Bimiralisib (PQR309)(free base);BIMIRALISIB;PQR309;PQR 309;PQR-309
CBNumber
CB73039400
Molecular Formula
C17H20F3N7O2
Formula Weight
411.38
MOL File
1225037-39-7.mol
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5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine Property

Boiling point:
643.7±65.0 °C(Predicted)
Density 
1.418±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:22.0(Max Conc. mg/mL);53.48(Max Conc. mM)
DMF:10.0(Max Conc. mg/mL);24.31(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);4.86(Max Conc. mM)
form 
A crystalline solid
pka
4.92±0.10(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.

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

P271Use only outdoors or in a well-ventilated area.

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

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

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.

P321Specific treatment (see … on this label).

P330Rinse mouth.

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
23441
Product name
Bimiralisib
Purity
≥98%
Packaging
1mg
Price
$36
Updated
2024/03/01
Cayman Chemical
Product number
23441
Product name
Bimiralisib
Purity
≥98%
Packaging
5mg
Price
$155
Updated
2024/03/01
Cayman Chemical
Product number
23441
Product name
Bimiralisib
Purity
≥98%
Packaging
10mg
Price
$290
Updated
2024/03/01
Cayman Chemical
Product number
23441
Product name
Bimiralisib
Purity
≥98%
Packaging
25mg
Price
$638
Updated
2024/03/01
ChemScene
Product number
CS-4672
Product name
Bimiralisib
Purity
98.74%
Packaging
100mg
Price
$640
Updated
2021/12/16
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5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine Chemical Properties,Usage,Production

Description

Bimiralisib is a potent and orally bioavailable inhibitor of phosphatidylinositol 3-kinases (PI3Ks; IC50s = 33, 661, 708, and 451 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively) and the mammalian target of rapamycin (mTOR; IC50 = 89 nM). It is selective for these kinases over a panel of cell surface and nuclear receptors, membrane channels, transporters, kinases, proteases, and phosphodiesterases at a concentration of 10 μM. Bimiralisib has anticancer activity with an average GI50 value of 0.7 μM across the National Cancer Institute (NCI) 60 human cancer cell line panel. In vivo, bimiralisib (5-15 mg/kg) reduces tumor growth in a dose-dependent manner in a PC3 prostate cancer mouse xenograft model. Formulations containing bimiralisib are under clinical investigation for the treatment of relapsed and refractory lymphoma and advanced solid tumors.

Uses

Bimiralisib is an orally bioavailable PI3K/mTOR inhibitor for cancer

in vivo

Oral administration yields similar concentrations of Bimiralisib in brain and plasma samples illustrates that Bimiralisib readily passes the blood–brain barrier. In mice, both po and iv application routes show a rapid drop below 200 ng/mL (~0.5 μM) of PQR309 within <1 h (iv) to <2 h (po) after administration, which reflects the time point when the drug reaches the median GI50 determined in tumor cell lines. In female rats a single oral dose (10 mg/kg) achieves similar drug levels as a single intravenous injection (5 mg/kg) with regard to Cmax. The half-life of 5-8 h and an AUC0.25-12 of around 14 000 h?ng/mL contributed to an excellent oral bioavailability of PQR309 (>50%). Twenty-four hours after po administration, plasma levels of PQR309 are still >2 μM (800-1000 ng/mL). Moreover, after 1-2 h exposure to PQR309 , drug levels in rat brain samples are comparable to plasma levels, confirming rapid access of PQR309 to the brain[1].

IC 50

PI3Kα: 33 nM (IC50); PI3Kα-H1047R: 36 nM (IC50); PI3Kα-E542K: 63 nM (IC50); PI3Kα-E545K: 136 nM (IC50); PI3Kδ: 451 nM (IC50); PI3Kβ: 661 nM (IC50); PI3Kγ: 708 nM (IC50); Vps34: 6486 nM (IC50); mTOR: 89 nM (IC50); mTORC1; mTORC2; DNA-PK: 8567 nM (IC50)

References

[1] FLORENT BEAUFILS. 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology[J]. Journal of Medicinal Chemistry, 2017, 60 17: 7524-7538. DOI: 10.1021/acs.jmedchem.7b00930

5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine Preparation Products And Raw materials

Raw materials

Preparation Products

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5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine Suppliers

China 85 India 2 United States 9 Global 96
Haoyuan Chemexpress Co., Ltd.
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021-58950125
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(86) 21-58955996
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ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185
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sales-cpd@caerulumpharma.com
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13621943973
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Shanghai Lollane Biological Technology Co.,Ltd.
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Guangzhou QiYun Biotechnology Co., Ltd.
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020-61288194 61288195
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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View Lastest Price from 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine manufacturers

Career Henan Chemical Co
Product
5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine 1225037-39-7
Price
US $1.00/KG
Min. Order
1KG
Purity
95%~99%
Supply Ability
per week 100kg
Release date
2019-09-05

1225037-39-7, 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amineRelated Search:

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  • 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine
  • PI3K-IN-2
  • PQR309
  • Bimiralisib
  • PQR309 Bimiralisib
  • CS-2024
  • PQR309;PQR 309;PQR-309
  • Bimiralisib (PQR309)(free base)
  • PQR-309, >98%
  • 2-Pyridinamine,5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)-
  • BIMIRALISIB;PQR309;PQR 309;PQR-309
  • Bimiralisib (PQR309)
  • 5-(4,6-Di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)-2-pyridinamine
  • 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine|||PQR309|||PI3K-IN-2
  • 1225037-39-7
  • C17H20F3N7O2
  • Inhibitors
  • APIs