Synonym
HLM006474; HLM-006474; HLM 006474;
IUPAC/Chemical Name
7-[(4-Ethoxy-3-methylphenyl)(2-pyridinylamino)methyl]-2-methyl-8-quinolinol
InChi Key
CYNZBLNMIJNBSF-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H25N3O2/c1-4-30-21-13-11-19(15-16(21)2)23(28-22-7-5-6-14-26-22)20-12-10-18-9-8-17(3)27-24(18)25(20)29/h5-15,23,29H,4H2,1-3H3,(H,26,28)
SMILES Code
OC1=C2N=C(C)C=CC2=CC=C1C(C3=CC=C(OCC)C(C)=C3)NC4=NC=CC=C4
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
In vitro activity:
To examine its effect on a range of commonly studied cell lines, this study utilized standard MTS assays to quantify cell viability following HLM006474 treatment. The results of these assays clearly indicate that HLM006474 decreases the number of viable cells over the experimental time course.
Reference: Cancer Res. 2008 Aug 1;68(15):6292-9. https://pubmed.ncbi.nlm.nih.gov/18676853/
In vivo activity:
To test this hypothesis, this study screened for compounds that might inhibit E2F DNA-binding and identified one small molecule that clearly targets E2F in vivo. In vivo this inhibitor leads to significant downregulation of E2F4 protein. This unexpected activity may account for the primary biological activity and specificity of HLM006474 and provides an easy way to monitor its biological activity (E2F4 western blotting or IHC).
Reference: Cancer Res. 2008 Aug 1;68(15):6292-9. https://pubmed.ncbi.nlm.nih.gov/18676853/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
25.0 |
62.58 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
399.49
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Ma Y, Kurtyka CA, Boyapalle S, Sung SS, Lawrence H, Guida W, Cress WD. A small-molecule E2F inhibitor blocks growth in a melanoma culture model. Cancer Res. 2008 Aug 1;68(15):6292-9. doi: 10.1158/0008-5472.CAN-08-0121. PMID: 18676853; PMCID: PMC3615411.
In vitro protocol:
1. Ma Y, Kurtyka CA, Boyapalle S, Sung SS, Lawrence H, Guida W, Cress WD. A small-molecule E2F inhibitor blocks growth in a melanoma culture model. Cancer Res. 2008 Aug 1;68(15):6292-9. doi: 10.1158/0008-5472.CAN-08-0121. PMID: 18676853; PMCID: PMC3615411.
In vivo protocol:
1. Ma Y, Kurtyka CA, Boyapalle S, Sung SS, Lawrence H, Guida W, Cress WD. A small-molecule E2F inhibitor blocks growth in a melanoma culture model. Cancer Res. 2008 Aug 1;68(15):6292-9. doi: 10.1158/0008-5472.CAN-08-0121. PMID: 18676853; PMCID: PMC3615411.
1: Huang T, Yang L, Wang G, Ding G, Peng B, Wen Y, Wang Z. Inhibition of Skp2 sensitizes lung cancer cells to paclitaxel. Onco Targets Ther. 2017 Jan 18;10:439-446. doi: 10.2147/OTT.S125789. eCollection 2017. PubMed PMID: 28176922; PubMed Central PMCID: PMC5261849.
2: Kurtyka CA, Chen L, Cress WD. E2F inhibition synergizes with paclitaxel in lung cancer cell lines. PLoS One. 2014 May 15;9(5):e96357. doi: 10.1371/journal.pone.0096357. eCollection 2014. PubMed PMID: 24831239; PubMed Central PMCID: PMC4022639.
3: Sangwan M, McCurdy SR, Livne-Bar I, Ahmad M, Wrana JL, Chen D, Bremner R. Established and new mouse models reveal E2f1 and Cdk2 dependency of retinoblastoma, and expose effective strategies to block tumor initiation. Oncogene. 2012 Nov 29;31(48):5019-28. doi: 10.1038/onc.2011.654. Epub 2012 Jan 30. PubMed PMID: 22286767; PubMed Central PMCID: PMC4977187.
4: Ma Y, Kurtyka CA, Boyapalle S, Sung SS, Lawrence H, Guida W, Cress WD. A small-molecule E2F inhibitor blocks growth in a melanoma culture model. Cancer Res. 2008 Aug 1;68(15):6292-9. doi: 10.1158/0008-5472.CAN-08-0121. PubMed PMID: 18676853; PubMed Central PMCID: PMC3615411.
