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AZD5438 - 10mM in DMSO, high purity , CAS No.602306-29-6(DMSO), Cyclin-dependent kinase inhibitor

COA

Grade & Purity:

Moligand™

10mM in DMSO

Cas Number: 602306-29-6(DMSO)
Molecular Weight: 371.46

In stock

Item Number

A409007

Grouped product items
SKU	Size	Availability	Price	Qty
A409007-1ml	1ml	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$206.90

CDK9 Selective Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)-N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine
Specifications & Purity	Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms	AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1.
Storage Temp	Store at -80°C
Shipped In	Dry ice packs + Cold packs This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Cyclin-dependent kinase inhibitor
Product Description	Information AZD5438 is a potent inhibitor ofCDK1/2/9withIC50of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1. In vitro AZD5438 exhibits the potent inhibitory effect on activity of cyclin-dependent kinases including cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, cyclin D3-cdk6, and cyclin T-cdk9 with IC50 of 6 nM, 45 nM, 16 nM, 21 nM, and 20 nM, respectively. Besides, AZD5438 also inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3β with IC50 of 14 nM and 17 nM, respectively. AZD5438 induces cell cycle arrest by inhibiting phosphorylation of cdk-dependent substrates, and exhibits the broad antiproliferative activity against a range of tumor cell lines including lung, colorectal, breast, prostate, and hematologic tumors with IC50 ranging from 0.2 μM (MCF-7) to 1.7 μM (ARH-77). In vivo In vivo, oral treatment of AZD5438 leads to statistically significant inhibition against the growth of human tumor xenografts derived from a wide range of different cancer types including breast, colon, lung, prostate, and ovarian with maximum TGI ranging from 38% to 153%. In the SW620 xenograft model, AZD5438 causes the inhibition of several cell cycle proteins such as, phH3, phosphonucleolin, PP1a, and several phospho-pRb epitopes in a dose-dependent manner. Cell Data cell lines：Panc-1 cells Concentrations：0 to 10 μM Incubation Time：48 hours or 72 hours Powder Purity:≥99%

Product Properties

ALogP	2.966
hba_count	5
HBD Count	1
Rotatable Bond	5

Associated Targets(Human)

CDK1 Tchem Cyclin-dependent kinase 1 (1 Activities)

Discover Target: CDK1

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

CCNE1 Tchem G1/S-specific cyclin-E1 (1 Activities)

Discover Target: CCNE1

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

CCNB1 Tchem G2/mitotic-specific cyclin-B1 (1 Activities)

Discover Target: CCNB1

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

CDK9 Tchem Cyclin-dependent kinase 9 (1 Activities)

Discover Target: CDK9

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

CCNA2 Tchem Cyclin-A2 (1 Activities)

Discover Target: CCNA2

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

CCND3 Tchem G1/S-specific cyclin-D3 (1 Activities)

Discover Target: CCND3

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

CCNT1 Tchem Cyclin-T1 (1 Activities)

Discover Target: CCNT1

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

CDK2 Tchem Cyclin-dependent kinase 2 (3 Activities)

Discover Target: CDK2

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

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (1 Activities)

Discover Target: KCNH2

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

Names and Identifiers

Smiles	CC(C)[N]1C(=NC=C1C2=NC(=NC=C2)NC3=CC=C(C=C3)[S](C)(=O)=O)C
Molecular Weight	371.46
Reaxy-Rn	14464752
Reaxys-RN_link_address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14464752&ln=

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

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

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro Water: 63 mg/mL (199.84 mM); DMSO: 2 mg/mL (6.34 mM); Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility	74
DMSO(mM) Max Solubility	199.21
Water(mg / mL) Max Solubility	<1

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