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PI-273 - ≥98.0%, high purity , CAS No.925069-34-7

    Grade & Purity:
  • ≥98%
In stock
Item Number
P647169
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P647169-1mg
1mg
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$80.90
P647169-5mg
5mg
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$160.90
P647169-10mg
10mg
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$270.90
P647169-25mg
25mg
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$550.90
P647169-50mg
50mg
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$900.90
P647169-100mg
100mg
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$1,500.90

Basic Description

Specifications & Purity ≥98%
Biochemical and Physiological Mechanisms PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC 50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC 50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis

In Vitro

PI-273 (2 μM; 48 hours) blocks the cell cycle at the G2-M phase. PI-273 (2 μM; 48 hours) induces cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3. PI-273 (0.5-2 μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner. PI-273 of 1 μM and 2 μM inhibits the cell proliferation of both MCF-7 and T-47D cells in a time-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: MCF-7, T-47D, SK-BR-3, MDA-MB-231, SUM229PE, Hs 578T cells Concentration: 2 μM Incubation Time: 48 hours Result: Blocked the cell cycle at the G2-M phase. Apoptosis AnalysisCell Line: MCF-7, T-47D, and SK-BR-3 cells Concentration: 2 μM Incubation Time: 48 hours Result: Induced cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3. Western Blot AnalysisCell Line: MCF-7 cells Concentration: 0.5, 1, 2 μM Incubation Time: For 3 days Result: Suppressed the AKT signaling pathway in a dose- and time-dependent manner.

In Vivo

PI-273 (intraperitoneal injection; 25 mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts . PI-273 (0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically); 0.08-5 hours) has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1% . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Eight-week-old male BALB/c nude mice with MCF-7 cell Dosage: 25 mg/kg Administration: Intraperitoneal injection; daily; 15 days Result: Suppressed the tumor volume and weight in the MCF-7 xenografts. Animal Model: Male Sprague-Dawley (SD) rats Dosage: 0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically) (Pharmacokinetic Study) Administration: Intravenously or intragastrically; 0.08, 0.16, 0.33, 0.67, 1, 1.5, 2, 3 and 5 hours Result: Has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%.

Form:Solid

IC50& Target:PI4KIIα 0.47 μM (IC 50 )

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Class Benzene and substituted derivatives
Subclass Benzoic acids and derivatives
Intermediate Tree Nodes Halobenzoic acids and derivatives
Direct Parent 4-halobenzoic acids and derivatives
Alternative Parents Thiophene carboxamides  Benzoyl derivatives  Chlorobenzenes  Aryl chlorides  Vinylogous amides  Heteroaromatic compounds  Thioureas  Primary carboxylic acid amides  Organooxygen compounds  Organonitrogen compounds  Organochlorides  Organic oxides  Hydrocarbon derivatives  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents 4-halobenzoic acid or derivatives - Benzoyl - Thiophene carboxamide - Thiophene carboxylic acid or derivatives - Chlorobenzene - Halobenzene - Aryl chloride - Aryl halide - Heteroaromatic compound - Vinylogous amide - Thiophene - Primary carboxylic acid amide - Carboxamide group - Thiourea - Organoheterocyclic compound - Carboxylic acid derivative - Organosulfur compound - Organooxygen compound - Organonitrogen compound - Organochloride - Organohalogen compound - Hydrocarbon derivative - Organic oxide - Organic nitrogen compound - Organic oxygen compound - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as 4-halobenzoic acids and derivatives. These are benzoic acids or derivatives carrying a halogen atom at the 4-position of the benzene ring.
External Descriptors Not available

Names and Identifiers

IUPAC Name 2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide
INCHI InChI=1S/C16H16ClN3O2S2/c1-3-11-8(2)24-15(12(11)13(18)21)20-16(23)19-14(22)9-4-6-10(17)7-5-9/h4-7H,3H2,1-2H3,(H2,18,21)(H2,19,20,22,23)
InChIKey MIERMBQDBLFAFW-UHFFFAOYSA-N
Smiles CCC1=C(SC(=C1C(=O)N)NC(=S)NC(=O)C2=CC=C(C=C2)Cl)C
Isomeric SMILES CCC1=C(SC(=C1C(=O)N)NC(=S)NC(=O)C2=CC=C(C=C2)Cl)C
PubChem CID 17168969
MeSH Entry Terms 2-(3-(4-chlorobenzoyl)thioureido)-4-ethyl-5-methylthiophene-3-carboxamide;PI-273
Molecular Weight 381.9

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : 6.02 mg/mL (15.76 mM; ultrasonic and warming and heat to 60°C)
Molecular Weight 381.900 g/mol
XLogP3 4.200
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 4
Exact Mass 381.037 Da
Monoisotopic Mass 381.037 Da
Topological Polar Surface Area 145.000 Ų
Heavy Atom Count 24
Formal Charge 0
Complexity 498.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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