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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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P647169-1mg
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1mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$80.90
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P647169-5mg
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5mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$160.90
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P647169-10mg
|
10mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$270.90
|
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P647169-25mg
|
25mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$550.90
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P647169-50mg
|
50mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$900.90
|
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P647169-100mg
|
100mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$1,500.90
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| 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 ) |
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 |
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| 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 |
| 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 |