Molecular structure of AZD 5438, CAS Number: 602306-29-6
AZD 5438 (CAS 602306-29-6)
Alternate Names:
AZD 5438 is also known as 4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine and N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine
Application:
AZD 5438 is an antiproliferative agent and potent inhibitor of cyclin-dependent kinases Cdk1, Cdk2, and Cdk9
CAS Number:
602306-29-6
Purity:
≥98%
Molecular Weight:
371.46
Molecular Formula:
C18H21N5O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
AZD 5438 is an antiproliferative agent and potent inhibitor of cyclin-dependent kinases Cdk1/cyclin B1 (IC50 = 16 nM), Cdk2/cyclin E (IC50 = 6 nM), Cdk2/cyclin A (IC50 = 45 nM), Cdk6/cyclin D3 (IC50 = 21 nM), and Cdk9/cyclin T (IC50 = 20 nM). AZD 5438 also inhibits the kinase activity of p25-cdk5 (IC50 = 14 nM) and glycogen synthase kinase 3β (IC50 = 17 nM). AZD 5438 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).
AZD 5438 (CAS 602306-29-6) References
- A first-in-man phase I tolerability and pharmacokinetic study of the cyclin-dependent kinase-inhibitor AZD5438 in healthy male volunteers. | Camidge, DR., et al. 2007. Cancer Chemother Pharmacol. 60: 391-8. PMID: 17115157
- A phase I pharmacodynamic study of the effects of the cyclin-dependent kinase-inhibitor AZD5438 on cell cycle markers within the buccal mucosa, plucked scalp hairs and peripheral blood mononucleocytes of healthy male volunteers. | Camidge, DR., et al. 2007. Cancer Chemother Pharmacol. 60: 479-88. PMID: 17143601
- Development of cell-cycle inhibitors for cancer therapy. | Dickson, MA. and Schwartz, GK. 2009. Curr Oncol. 16: 36-43. PMID: 19370178
- AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. | Byth, KF., et al. 2009. Mol Cancer Ther. 8: 1856-66. PMID: 19509270
- Safety, tolerability, pharmacokinetics and pharmacodynamics of the oral cyclin-dependent kinase inhibitor AZD5438 when administered at intermittent and continuous dosing schedules in patients with advanced solid tumours. | Boss, DS., et al. 2010. Ann Oncol. 21: 884-894. PMID: 19825886
- AZD5438, an inhibitor of Cdk1, 2, and 9, enhances the radiosensitivity of non-small cell lung carcinoma cells. | Raghavan, P., et al. 2012. Int J Radiat Oncol Biol Phys. 84: e507-14. PMID: 22795803
- Detection of tyrosine kinase inhibitors-induced COX-2 expression in bladder cancer by fluorocoxib A. | Bourn, J., et al. 2019. Oncotarget. 10: 5168-5180. PMID: 31497247
- Requirement of cyclin-dependent kinase function for hepatitis B virus cccDNA synthesis as measured by digital PCR. | Bao, CY., et al. 2020. Ann Hepatol. 19: 280-286. PMID: 31964596
- Induction of cell cycle arrest and apoptosis in mantle cell lymphoma by AZD5438, a novel cyclin-dependent kinase inhibitor[J]. | Lo W C, Growcott J, LeBrun D P. 2010,. Cancer Research,. 70(8_Supplement):: 3890-3890.
- Inhibitory effect of the CDK4/6 inhibitor, PD 0332991, is enhanced by mTOR inhibition in Non-Small Cell Lung Cancer (NSCLC)[J]. | Gopalan P K, Gordillo-Villegas A, Zajac-Kaye M,. 2013,. Cancer Research,. 73(8_Supplement):: 693-693.
Inhibitor of:
1300002E11Rik, 1700018G05Rik, 4933404M19Rik, 4933411G11Rik, ALS2CR7, ANKRD20A1, ANKRD20A3, BC024659, BEND6, Beta-NAP, C12orf50_1700017N19Rik, C6orf1, CCDC77, CCNJL, Cdc123, CDCrel-1, Cdk1, Cdk2, Cdk9, CdkL4, CINP, Clb3, CNTD1, CPAN, cyclin A, cyclin A-type, cyclin B, cyclin B1, cyclin C, cyclin D1, cyclin E, cyclin E2, cyclin I, cyclin J, cyclin M2, cyclin Y, cyclin YL1, cyclin YL3, D-type cyclin, D14Ertd449e, Dcpp2, DOC1, E2F-3, E2F-7, EG624855, FAM127B, Gm75, Gtlf3b, HST, INCA1, Inv, KBP, Kin28, KKIALRE, KPRP, LOC341346, Mcpr1, MPc3_CBX8, MYT1L, NIF3L1 BP1, Nim1, Olfr971, p14 ARF/p16, p57, PCTAIRE-3, Peregrin, PISSLRE, PITSLRE A, PRRT4, Rad9B, RasGRP1, ROGDI, SERTAD4, Speedy E6, TEX27, TMEM194, Trav7-1, TSGA10IP, V1RG1, WDR66, ZFP260, ZHX3, ZNF20, and ZSCAN16.Activator of:
BUBR1, Cables1, CCRK, Cdc28, Cdk3, Cks1, Clb2, cyclin E, PISSLRE, PITSLRE B, and TRβ2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AZD 5438, 10 mg | sc-361115 | 10 mg | $205.00 | |||
AZD 5438, 50 mg | sc-361115A | 50 mg | $865.00 |