AZD 5438An antiproliferative agent and potent inhibitor of cyclin-dependent kinases Cdk1, Cdk2, and Cdk9

AZD 5438 (CAS 602306-29-6)

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Synonym: 4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
Application: 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
* Refer to Certificate of Analysis for lot specific data (including water content).
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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). AZD5438 also inhibits the kinase activity of p25-cdk5 (IC50 = 14 nM) and glycogen synthase kinase 3β (IC50 = 17 nM). 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).


References

1. Camidge, D.R. et al. 2007. Cancer Chemother. Pharmacol. 60(3): 391-398. PMID: 17115157
2. Camidge, D.R. et al. 2007. Cancer Chemother. Pharmacol. 60(4): 479-488. PMID: 17143601
3. Dickson, M.A. and Schwartz, G.K. 2009. Curr Oncol. 16(2): 36-43. PMID: 19370178
4. Byth, K.F. et al. 2009. Mol. Cancer Ther. 8(7): 1856-1866. PMID: 19509270
5. Boss, D.S. et al. 2010. Ann. Oncol. 21(4): 884-894. PMID: 19825886
6. Raghavan, P. et al. 2012. Int J Radiat Oncol Biol Phys. PMID: 22795803

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), water (<1 mg/ml) at 25 °C, and ethanol (74 mg/ml) at 25 °C.
Storage :
Desiccate at room temperature
Melting Point :
246.01° C (Predicted)
Boiling Point :
655.2±65.0° C at 760 mmHg
Density :
1.3±0.1 g/cm3
Refractive Index :
n20D 1.65 (Predicted)
IC50 :
cyclin-dependent kinase (cdk)1: IC50 = 16 nM; cyclin-dependent kinase (cdk)2: IC50 = 6 nM; cyclin-dependent kinase (cdk)9: IC50 = 20 nM; kinase activity of p25-cdk5: IC50 = 14 nM; glycogen synthase kinase 3β: IC50 = 17 nM; antiproliferative activity: IC50 = 0.2 µM (MCF-7); antiproliferative activity: IC50 = 1.7 µM (ARH-77); Cyclin T1: IC50 = 20 nM (human); G1/S-specific cyclin D3: IC50 = 21 nM (human); Cyclin A2: IC50 = 45 nM (human)
pK Values :
pKb: 4.08 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
16747683
MDL Number :
MFCD11112135
SMILES :
CC1=NC=C(N1C(C)C)C2=NC(=NC=C2)NC3=CC=C(C=C3)S(=O)(=O)C

Download SDS (MSDS)

Certificate of Analysis

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What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. AZD 5438, sc-361115, is an off-white solid.
Answered by: Chemical Support 4
Date published: 2017-04-26

What is the solubility?

Asked by: SCM4
AZD 5438 is soluble in Soluble in DMSO (100 mM), water (&lt;1 mg/ml) at 25 &deg;C, and ethanol (74 mg/ml) at 25 &deg;C. This information can also be found in the Technical Information tab.
Answered by: Tech Service 11
Date published: 2017-02-27
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