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XL413 hydrochloride

Cdc7 inhibitor CAS# 1169562-71-3

XL413 hydrochloride

Catalog No. BCC4039----Order now to get a substantial discount!

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Chemical structure

XL413 hydrochloride

3D structure

Chemical Properties of XL413 hydrochloride

Cas No. 1169562-71-3 SDF Download SDF
PubChem ID 67185304 Appearance Powder
Formula C14H13Cl2N3O2 M.Wt 326.18
Type of Compound N/A Storage Desiccate at -20°C
Synonyms BMS 863233
Solubility Soluble to 20 mM in water
Chemical Name 8-chloro-2-[(2S)-pyrrolidin-2-yl]-1H-[1]benzofuro[3,2-d]pyrimidin-4-one;hydrochloride
SMILES C1CC(NC1)C2=NC(=O)C3=C(N2)C4=C(O3)C=CC(=C4)Cl.Cl
Standard InChIKey UNDKJUKLBNARIZ-FVGYRXGTSA-N
Standard InChI InChI=1S/C14H12ClN3O2.ClH/c15-7-3-4-10-8(6-7)11-12(20-10)14(19)18-13(17-11)9-2-1-5-16-9;/h3-4,6,9,16H,1-2,5H2,(H,17,18,19);1H/t9-;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of XL413 hydrochloride

DescriptionPotent and selective Cdc7 inhibitor (IC50 = 3.4 nM). Exhibits >12-fold selectivity for Cdc7 over PIM-1 kinase and >30-fold selectivity over pMCM and CK2. Inhibits proliferation of Colo 205 cells in vitro and attenuates tumor growth of Colo 205 xenografts in mice.

XL413 hydrochloride Dilution Calculator

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XL413 hydrochloride Molarity Calculator

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Preparing Stock Solutions of XL413 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.0658 mL 15.329 mL 30.6579 mL 61.3158 mL 76.6448 mL
5 mM 0.6132 mL 3.0658 mL 6.1316 mL 12.2632 mL 15.329 mL
10 mM 0.3066 mL 1.5329 mL 3.0658 mL 6.1316 mL 7.6645 mL
50 mM 0.0613 mL 0.3066 mL 0.6132 mL 1.2263 mL 1.5329 mL
100 mM 0.0307 mL 0.1533 mL 0.3066 mL 0.6132 mL 0.7664 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on XL413 hydrochloride

XL413 is a potent and selective Cdc7 inhibitor with an IC50 of 3.7 nM, >60-fold selectivity against CK2, >10-fold selectivity against PIM, and >300-fold selectivity against a panel of over 100 protein kinases. Phase 1

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References on XL413 hydrochloride

The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds.[Pubmed:25412417]

PLoS One. 2014 Nov 20;9(11):e113300.

Cdc7-Dbf4 kinase or DDK (Dbf4-dependent kinase) is required to initiate DNA replication by phosphorylating and activating the replicative Mcm2-7 DNA helicase. DDK is overexpressed in many tumor cells and is an emerging chemotherapeutic target since DDK inhibition causes apoptosis of diverse cancer cell types but not of normal cells. PHA-767491 and XL413 are among a number of potent DDK inhibitors with low nanomolar IC50 values against the purified kinase. Although XL413 is highly selective for DDK, its activity has not been extensively characterized on cell lines. We measured anti-proliferative and apoptotic effects of XL413 on a panel of tumor cell lines compared to PHA-767491, whose activity is well characterized. Both compounds were effective biochemical DDK inhibitors but surprisingly, their activities in cell lines were highly divergent. Unlike PHA-767491, XL413 had significant anti-proliferative activity against only one of the ten cell lines tested. Since XL413 did not effectively inhibit DDK in multiple cell lines, this compound likely has limited bioavailability. To identify potential leads for additional DDK inhibitors, we also tested the cross-reactivity of approximately 400 known kinase inhibitors against DDK using a DDK thermal stability shift assay (TSA). We identified 11 compounds that significantly stabilized DDK. Several inhibited DDK with comparable potency to PHA-767491, including Chk1 and PKR kinase inhibitors, but had divergent chemical scaffolds from known DDK inhibitors. Taken together, these data show that several well-known kinase inhibitors cross-react with DDK and also highlight the opportunity to design additional specific, biologically active DDK inhibitors for use as chemotherapeutic agents.

Discovery of XL413, a potent and selective CDC7 inhibitor.[Pubmed:22560567]

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31.

CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell lines, with inhibition of CDC7 resulting in cell cycle arrest. In this paper, we disclose the discovery of a potent and selective CDC7 inhibitor, XL413 (14), which was advanced into Phase 1 clinical trials. Starting from advanced lead 3, described in a preceding communication, we optimized the CDC7 potency and selectivity to demonstrate in vitro CDC7 dependent cell cycle arrest and in vivo tumor growth inhibition in a Colo-205 xenograft model.

Description

Potent and selective Cdc7 inhibitor,XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, showing 63-, 12- and 35-fold selectivity over CK2, Pim-1 and pMCM2, respectively. Phase 1/2.

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