HLM006474
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 562972

CAS#: 353519-63-8

Description: HLM006474 is a pan-E2F inhibitor. It inhibits DNA binding to E2F1, E2F2, and E2F4 in A375 melanoma cells when used at a concentration of 40 µM.

Chemical Structure

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HLM006474
CAS# 353519-63-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 562972
Name: HLM006474
CAS#: 353519-63-8
Chemical Formula: C25H25N3O2
Exact Mass: 399.19
Molecular Weight: 399.490
Elemental Analysis: C, 75.16; H, 6.31; N, 10.52; O, 8.01

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1350 Ready to ship
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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

Appearance: Solid powder

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

More Info:

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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25.0 62.58

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.

Recalculate based on batch purity %
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.

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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.