PIK-75 Hydrochloride

Product Name: PIK-75 Hydrochloride
CAS No.: 372196-77-5
Chemical Name: PIK-75 Hydrochloride
Synonyms: PFK-15;CS-434;PIK-75 HCl;PIK-75;PIK 75;PIK-75 HYDROCHLORIDE; PIK 75;PIK-75 HCl PI 3-Kα Inhibitor VIII;(E)-N'-((6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydraz;N'-((6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride;N'-((6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride;2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride
CBNumber: CB92561492
Molecular Formula: C16H15BrClN5O4S
Formula Weight: 488.7434
MOL File: 372196-77-5.mol

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PIK-75 Hydrochloride Property

Melting point:: >156°C (dec.)
storage temp.: Inert atmosphere,Store in freezer, under -20°C
solubility: DMSO (Slightly), Methanol (Slightly)
form: Solid
color: Light Beige to Beige

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

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

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

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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

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

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 10009210
Product name: PIK-75 (hydrochloride)
Purity: ≥98%
Packaging: 1mg
Price: $25
Updated: 2024/03/01

Cayman Chemical

Product number: 10009210
Product name: PIK-75 (hydrochloride)
Purity: ≥98%
Packaging: 5mg
Price: $61
Updated: 2024/03/01

Cayman Chemical

Product number: 10009210
Product name: PIK-75 (hydrochloride)
Purity: ≥98%
Packaging: 10mg
Price: $84
Updated: 2024/03/01

Cayman Chemical

Product number: 10009210
Product name: PIK-75 (hydrochloride)
Purity: ≥98%
Packaging: 25mg
Price: $176
Updated: 2024/03/01

Tocris

Product number: 5339
Product name: PFK15
Purity: ≥99%(HPLC)
Packaging: 50
Price: $609
Updated: 2021/12/16

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PIK-75 Hydrochloride Chemical Properties,Usage,Production

Uses

PFK 15 is a novel inhibitor of glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). It suppresses the glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and induces apoptosis in abnormal cells.

Biological Activity

pik-75 is a specific inhibitor of p110α isoform of pi3k with ic50 of 5.8 nm [1].in acute myeloid leukemia cells, pik-75 targeted the p110α isoform of pi3k, which led to a loss of connection between bcl-xl and bak. pik-75 also transiently decreased cdk7/9, leading to loss of mcl-1 protein, and alleviation of its inhibition of pro-apoptotic bak. the simultaneous loss of bcl-xl and mcl-1 led to rapid apoptosis. [2] in human monocyte-endothelial cell, pik-75 suppressed the events of downstream signaling, including akt phosphorylation, ikk activation, and nf-kb transcription. pik-75 inhibited in vitro and in vivo production of tnf-α and il-6, decreased the e-selectin, icam-1, and vcam-1 expression, and blocked cell adhesion [3]. in human smooth muscle cells, pik-75 decreased tnf-α-induced cd38 expression in asthmatic and nonasthmatic cells [4]. in pancreatic β-cells, acute treatment with pik-75 enhanced the glucose-induced insulin secretion [5].

in vivo

pik-75 significantly suppressed the histological abnormalities associated with dextran sulfate sodium-induced murine colitis. pik-75 can attenuate experimental inflammation in the colon [3].

target

p110α

References

[1]. zheng z, amran si, thompson pe, jennings ig. isoform-selective inhibition of phosphoinositide 3-kinase: identification of a new region of nonconserved amino acids critical for p110α inhibition. mol pharmacol. 2011 oct;80(4):657-64.
[2]. thomas d, powell ja, vergez f, segal dh, nguyen ny, baker a, teh tc, barry ef, sarry je, lee em, nero tl, jabbour am, pomilio g, green bd, manenti s, glaser sp, parker mw, lopez af, ekert pg, lock rb, huang dc, nilsson sk, récher c, wei ah, guthridge ma. targeting acute myeloid leukemia by dual inhibition of pi3k signaling and cdk9-mediated mcl-1 transcription. blood. 2013 aug 1;122(5):738-48.
[3]. dagia nm, agarwal g, kamath dv, chetrapal-kunwar a, gupte rd, jadhav mg, dadarkar ss, trivedi j, kulkarni-almeida aa, kharas f, fonseca lc, kumar s, bhonde mr. a preferential p110alpha/gamma pi3k inhibitor attenuates experimental inflammation by suppressing the production of proinflammatory mediators in a nf-kappab-dependent manner. am j physiol cell physiol. 2010 apr;298(4):c929-41.
[4]. jude ja, tirumurugaan kg, kang bn, panettieri ra, walseth tf, kannan ms. regulation of cd38 expression in human airway smooth muscle cells: role of class i phosphatidylinositol 3 kinases. am j respir cell mol biol. 2012 oct;47(4):427-35.
[5]. aoyagi k, ohara-imaizumi m, nishiwaki c, nakamichi y, ueki k, kadowaki t, nagamatsu s. acute inhibition of pi3k-pdk1-akt pathway potentiates insulin secretion through upregulation of newcomer granule fusions in pancreatic β-cells. plos one. 2012;7(10):e47381.

PIK-75 Hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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PIK-75 Hydrochloride Suppliers

China 74 India 2 United Kingdom 1 United States 19 Global 96

AdooQ BioScience, LLC

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Cckinase, Inc.

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BOC Sciences

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View Lastest Price from PIK-75 Hydrochloride manufacturers

Career Henan Chemical Co

Product: PIK-75 Hydrochloride 372196-77-5
Price: US $1.00/g
Min. Order: 100EA
Purity: 99%
Supply Ability: G/KG/T
Release date: 2019-12-20

372196-77-5, PIK-75 HydrochlorideRelated Search:

PIK-93 PIK-294 N-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide Sulfanilic acid Benzoic acid Metanilic acid Alpelisib (BYL719) Pictilisib CAL-101 Flavopiridol (Alvocidib) HCl 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- BEZ235 (NVP-BEZ235, Dactolisib)

2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride

PFK-15

(E)-N'-((6-bromoH-imidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride

2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride PIK-75

Benzenesulfonic acid, 2-methyl-5-nitro-, 2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide, hydrochloride (1:1)

PIK-75;PIK 75

(E)-N'-((6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydraz

PIK-75 HCl

PIK-75 HYDROCHLORIDE; PIK 75

CS-434

N'-((6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride

PIK-75 HCl PI 3-Kα Inhibitor VIII

N'-((6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride

372196-77-5

C16H14BrN5O4SHCl

C16H15BrClN5O4S

Inhibitors

Akt

mTOR

PI3K

Antineoplastic