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KU-0060648 - 98% , high purity , CAS No.881375-00-4, Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit delta;Inhi

Moligand™
≥98%

CAS#: 881375-00-4
Formula: C₃₃H₃₄N₄O₄S
Molecular Weight: 582.71
PubChem CID: 11964036

Item Number

K129743

Grouped product items
SKU	Size	Availability	Price
K129743-1mg	1mg	In stock	$69.90
K129743-2mg	2mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$126.90
K129743-5mg	5mg	In stock	$147.90
K129743-10mg	10mg	In stock	$246.90
K129743-25mg	25mg	In stock	$543.90
K129743-50mg	50mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$979.90
K129743-100mg	100mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$1,762.90

Dual DNA-PK and PI 3-K inhibitor

View related series

phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit alpha Inhibitor phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit beta Inhibitor phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit delta Inhibitor phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit gamma Inhibitor protein kinase，DNA-activated，catalytic subunit Inhibitor

Basic Description

Synonyms	KU-0060648\|881375-00-4\|KU 0060648\|ku0060648\|LM6DZS6PYA\|2-(4-ethylpiperazin-1-yl)-N-[4-(2-morpholin-4-yl-4-oxochromen-8-yl)dibenzothiophen-1-yl]acetamide\|CHEMBL1086377\|2-(4-ethylpiperazin-1-yl)-N-(4-(2-morpholino-4-oxo-4H-chromen-8-yl)dibenzo[b,d]thiophen-
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	Dual PI 3-K and DNA-PK inhibitor (IC50values are <0.1, 0.5, 4 and 19 nM for PI 3-Kδ, PI 3-Kβ, PI 3-Kαand DNA-PK respectively). Inhibits proliferation of MCF7 cellsin vitroand delays growth of MCF7 xenografts in mice. Also enhances CRISPR-Cas9-mediated hom
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit delta;Inhi
Note	2mg卖完停产，不再备货

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

Discover Target: CYP2D6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

Discover Target: CYP2C19

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Discover Target: CYP3A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

Discover Target: CYP2C9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKDC Tchem DNA-dependent protein kinase catalytic subunit 6 Activities

Discover Target: PRKDC

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1 Activities

Discover Target: PIK3CG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 2 Activities

Discover Target: PIK3CA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIK3CB Tchem Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 2 Activities

Discover Target: PIK3CB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIK3CD Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1 Activities

Discover Target: PIK3CD

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ATR Tchem Serine/threonine-protein kinase ATR 0 Activities

Discover Target: ATR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKB Tchem Aurora kinase B 0 Activities

Discover Target: AURKB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ATM Tchem Serine-protein kinase ATM 0 Activities

Discover Target: ATM

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MTOR Tclin Serine/threonine-protein kinase mTOR 0 Activities

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	2-(4-ethylpiperazin-1-yl)-N-[4-(2-morpholin-4-yl-4-oxochromen-8-yl)dibenzothiophen-1-yl]acetamide
INCHI	InChI=1S/C33H34N4O4S/c1-2-35-12-14-36(15-13-35)21-29(39)34-26-11-10-23(33-31(26)25-6-3-4-9-28(25)42-33)22-7-5-8-24-27(38)20-30(41-32(22)24)37-16-18-40-19-17-37/h3-11,20H,2,12-19,21H2,1H3,(H,34,39)
InChi Key	AATCBLYHOUOCTO-UHFFFAOYSA-N
Canonical SMILES	CCN1CCN(CC1)CC(=O)NC2=C3C4=CC=CC=C4SC3=C(C=C2)C5=CC=CC6=C5OC(=CC6=O)N7CCOCC7
Isomeric SMILES	CCN1CCN(CC1)CC(=O)NC2=C3C4=CC=CC=C4SC3=C(C=C2)C5=CC=CC6=C5OC(=CC6=O)N7CCOCC7
Alternate CAS	881375-00-4
PubChem CID	11964036
MeSH Entry Terms	2-(4-ethylpiperazin-1-yl)-N-(4-(2-morpholino-4-oxo-4H-chromen-8-yl)dibenzo(b,d)thiophen-1-yl)acetamide;KU-0060648
Molecular Weight	582.71

Certificates

Certificate of Analysis(COA)

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To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

7 results found

Lot Number	Certificate Type	Date	Item
A2205559	Certificate of Analysis	Oct 10, 2023	K129743
A2205560	Certificate of Analysis	Oct 10, 2023	K129743
A2205561	Certificate of Analysis	Oct 10, 2023	K129743
A2205562	Certificate of Analysis	Oct 10, 2023	K129743
A2205563	Certificate of Analysis	Oct 10, 2023	K129743
A2205564	Certificate of Analysis	Oct 10, 2023	K129743
A2205565	Certificate of Analysis	Oct 10, 2023	K129743

References

1. Munck JM, Batey MA, Zhao Y, Jenkins H, Richardson CJ, Cano C, Tavecchio M, Barbeau J, Bardos J, Cornell L et al.. (2012) Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K.. Mol Cancer Ther, 11 (8): (1789-98). [PMID:22576130]
2. Cano C, Saravanan K, Bailey C, Bardos J, Curtin NJ, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Menear KA et al.. (2013) 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.. J Med Chem, 56 (16): (6386-401). [PMID:23855836]

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