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 C_max. The half-life of 5-8 h and an AUC_0.25-12 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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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:

PPQ-102 IGF-1R Inhibitor II, N-(5-Chloro-2-methoxyphenyl)-Nμ-(2-methylquinolin-4-yl)urea PQR620 PQR530

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