CP-10 - ≥98% , CAS No.2366268-80-4

CAS: 2366268-80-4 Cat. No.: C650023 Summenformel: C₄₄H₄₉N₁₃O₇ Molekulargewicht: 871.94 EG-Nummer: 958-152-7 PubChem CID: 138911323

GRADE & PURITY ≥98%

Storage

Store at -20°C,Argon charged

Shipped In

Ice chest + Ice pads

Application

PROTAC

Übersicht

CP-10 is a PROTAC connected by ligands for Cereblon and CDK , with highly selective, specific, and remarkable CDK6 degradation ( DC 50 =2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6

In Vitro

CP-10 induces nearly 72% degradation of CDK6 at 10 nM and 89% at 100 nM in human glioblastoma U251 cells. The degradation of CDK4 induced by CP-10 is far weaker than that of CDK6 (DC 50 : 50-80 fold). ?\nCP-10 displays a cell inhibition potential in multiple myeloma cell MM.1S (IC 50 ≈10 nM) and mantle cell lymphoma cells (in Mino, IC 50 ≈8 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:CDK6 2.1 nM (DC 50 ) Cereblon

Specifications

Spezifikationen & Reinheit

≥98%

Biochemische und physiologische Mechanismen

CP-10 is a PROTAC connected by ligands for Cereblon and CDK , with highly selective, specific, and remarkable CDK6 degradation ( DC 50 =2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple my

Storage

Store at -20°C,Argon charged

Verschickt in

Ice chest + Ice pads

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Reinheit

≥98%

Namen und Kennungen

• Kanonisches Lächeln: CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCN(CC4)CC5=CN(N=N5)CCOCCNC6=CC=CC7=C6C(=O)N(C7=O)C8CCC(=O)NC8=O)C9CCCC9)C(=O)C
• IUPAC Name: 4-[2-[2-[4-[[4-[6-[(6-acetyl-8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]pyridin-3-yl]piperazin-1-yl]methyl]triazol-1-yl]ethoxy]ethylamino]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
• InChIKey: PACRWHUPEPCFHX-UHFFFAOYSA-N
• INCHI: 1S/C44H49N13O7/c1-26-32-23-47-44(50-39(32)56(29-6-3-4-7-29)42(62)37(26)27(2)58)48-35-12-10-30(22-46-35)54-17-15-53(16-18-54)24-28-25-55(52-51-28)19-21-64-20-14-45-33-9-5-8-31-38(33)43(63)57(41(31)61)34-11-13-36(59)49-40(34)60/h5,8-10,12,22-23,25,29,34,45H,3-4,6-7,11,13-21,24H2,1-2H3,(H,49,59,60)(H,46,47,48,50)
• Isomere SMILES: CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCN(CC4)CC5=CN(N=N5)CCOCCNC6=CC=CC7=C6C(=O)N(C7=O)C8CCC(=O)NC8=O)C9CCCC9)C(=O)C
• PubChem CID: 138911323
• MeSH-Eintrag: CP-10;quinterenol;quinterenol monohydrochloride;quinterenol monohydrochloride, (+-)-isomer;quinterenol sulfate (2:1);quinterenol, (+-)-isomer;quinterenol, dihydrochloride
• Molekulargewicht: 871.94

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Organoheterocyclic compounds
    • Klasse Diazinanes
      • Subclass Piperazines

• Kingdom: Organic compounds
• Superclass: Organoheterocyclic compounds
• Klasse: Diazinanes
• Subclass: Piperazines
• Intermediate Tree Nodes: Not available
• Direct Parent: Pyridinylpiperazines
• Alternative Parents: N-arylpiperazines Phthalimides Pyrido[2,3-d]pyrimidines Alpha amino acids and derivatives Isoindoles Piperidinediones Dialkylarylamines Aryl alkyl ketones Secondary alkylarylamines Pyridinones N-alkylpiperazines Methylpyridines Delta lactams Aralkylamines Aminopyrimidines and derivatives Aminopyridines and derivatives N-substituted carboxylic acid imides Imidolactams Benzenoids Vinylogous amides Triazoles N-unsubstituted carboxylic acid imides Heteroaromatic compounds Dicarboximides Trialkylamines Dialkyl ethers Azacyclic compounds Organopnictogen compounds Organic oxides Hydrocarbon derivatives
• Molecular Framework: Aromatic heteropolycyclic compounds
• Substituents: N-arylpiperazine - Pyridinylpiperazine - Phthalimide - Pyrido[2,3-d]pyrimidine - Pyridopyrimidine - Isoindolone - Alpha-amino acid or derivatives - Isoindole or derivatives - Isoindole - Isoindoline - Dialkylarylamine - Aryl alkyl ketone - Aryl ketone - Tertiary aliphatic/aromatic amine - Piperidinedione - Methylpyridine - Aralkylamine - N-alkylpiperazine - Secondary aliphatic/aromatic amine - Pyridinone - Piperidinone - Delta-lactam - Aminopyrimidine - Aminopyridine - Imidolactam - Benzenoid - Pyrimidine - Pyridine - Piperidine - Carboxylic acid imide, n-substituted - Heteroaromatic compound - Vinylogous amide - 1,2,3-triazole - Carboxylic acid imide, n-unsubstituted - Dicarboximide - Carboxylic acid imide - Azole - Tertiary aliphatic amine - Tertiary amine - Lactam - Ketone - Amino acid or derivatives - Azacycle - Secondary amine - Ether - Dialkyl ether - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Carbonyl group - Amine - Aromatic heteropolycyclic compound
• Beschreibung: This compound belongs to the class of organic compounds known as pyridinylpiperazines. These are compounds containing a pyridinylpiperazine skeleton, which consists of a pyridine linked (not fused) to a piperazine by a bond by a single bond that is not part of a ring.
• External Descriptors: Not available

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

Zugehörige Ziele (menschlich)

CDK6 Tclin Cyclin-dependent kinase 6 (1724 Activities)

Discover Target: CDK6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HL-60 (67320 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MCF7 (126967 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

RPMI-8226 (44974 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

THP-1 (11052 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

JeKo-1 (376 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MM1.S (1111 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MAP2K7 Tchem Protein cereblon/MAP2K7 (2 Activities)

Discover Target: MAP2K7

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

EGFR Tclin Protein cereblon/Epidermal growth factor receptor (191 Activities)

Discover Target: EGFR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK1 Tchem Protein cereblon/Cyclin-dependent kinase 1 (7 Activities)

Discover Target: CDK1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK4 Tclin Protein cereblon/Cyclin-dependent kinase 4 (68 Activities)

Discover Target: CDK4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CCND1 Tchem Protein cereblon/G1/S-specific cyclin-D1 (1 Activities)

Discover Target: CCND1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK2 Tchem Protein cereblon/Cyclin-dependent kinase 2 (25 Activities)

Discover Target: CDK2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK9 Tchem Protein cereblon/CDK9 (113 Activities)

Discover Target: CDK9

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK6 Tclin Protein cereblon/Cyclin-dependent kinase 6 (113 Activities)

Discover Target: CDK6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK5 Tchem Protein cereblon/Cyclin-dependent-like kinase 5 (8 Activities)

Discover Target: CDK5

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MAP2K1 Tclin Protein cereblon/MAP2K1 (15 Activities)

Discover Target: MAP2K1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Wirkungsmechanismen

Chemische und physikalische Eigenschaften

• Löslichkeit: DMSO : 200 mg/mL (229.37 mM; Need ultrasonic)

Häufig gestellte Fragen

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C under argon. It is supplied under an argon blanket; reseal under inert gas after each use.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2366268-80-4, the molecular formula is C44H49N13O7, and the molecular weight is 871.94 g/mol. InChIKey PACRWHUPEPCFHX-UHFFFAOYSA-N.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.