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AZD5438

AZD5438

Item no.	S2621-1000
Manufacturer	Selleckchem
CASRN	602306-29-6
Amount	1 g
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 50 mg 5 g
Category	Oncology Neuroscience Metabolism Cholesterol & Lipid Metabolism Neural Signaling Enzymes Other Fatty Acid Enzymes Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Colorectal Cancer Breast Cancer Testicular & Prostate Cancer Lymphatic System Cancer Uterine, Ovarian & Cervical Cancer
Type	Inhibitors
Specific against	other
Smiles	CC1=NC=C(N1C(C)C)C2=NC(=NC=C2)NC3=CC=C(C=C3)S(=O)(=O)C
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	602306-29-6 '
Similar products	AZD5438
Available
Manufacturer - Targets	CDK9, CDK2, CDK1
Storage Conditions	2 years -80 in solvent
Molecular Weight	371, 46
Administration	Administered via p.o.
Animal Models	MCF-7, HCT-116, A549, and IM-9 cells are injected s.c. into the Swiss nude mice and nude rats.
Cell lines	MCF-7, HCT-116, A549, and IM-9
Clinical Trials	Study on AZD5438 has been completed in Phase I clinical trials in patients with Advanced Solid Malignancies.
Concentrations	0 to 10 uM
Dosages	<=100 mg/kg
Formulation	AZD5438 is dissolved in hydroxy-propyl-methyl-cellulose.
IC50	16 nM [1], 16 nM [1], 16 nM [1], 16 nM [1], 16 nM [1], 16 nM [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 3beta with IC50 of 14 nM and 17 nM, respectively. [1] 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 uM (MCF-7) to 1.7 uM (ARH-77). [1]
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%. [1] 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. [1]
Incubation Time	48 hours or 72 hours
Method	AZD5438 is tested against solid tumor cell lines. Briefly, cells are incubated for 48 hours with AZD5438 at a range of concentrations. At the end of incubation, the cells are pulsed with 5-bromo-2 -deoxyuridine (BrdUrd) and the amount of DNA synthesis is measured. The IC50 for inhibition of proliferation is specifically determined independently of cell death. Multiple myeloma cell lines are seeded into 96-well plates in RPMI 1640 supplemented with 10% FCS and glutamine and dosed with AZD5438 for 72 hours. Cell growth is measured using AlamarBlue and GI50 values are calculated with reference to pretreatment control values.
Solubility (25C)	DMSO 74 mg/mL, Water <1 mg/mL, Ethanol 74 mg/mL
Information	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.
Chemical Name	4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)-N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine
Features	AZD5438 is a potent inhibitor of cyclin-dependent kinase (cdk) 1, 2, and 9.

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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S2621-1000-datasheet.pdf

S2621-1000-safety-datasheet.pdf