DACA

Name: DACA
Brand: MedChemExpress
SKU: HY-100777
Rating: 4.5 (0 reviews)

Cat. No.: HY-100777 Purity: 98.89%: Data Sheet
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DACA (XR 5000) is a potential and blood-brain barrier-penetrating topoisomerase I and II inhibitor. DACA can be used in the research of colorectal cancer, leukemia and lung cancer.

For research use only. We do not sell to patients.

DACA Chemical Structure

CAS No. : 89459-25-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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DACA (Standard) Get quote

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Topoisomerase Topo I Topo II DNA gyrase

Biological Activity
Purity & Documentation
References
Customer Review

Description

DACA (XR 5000) is a potential and blood-brain barrier-penetrating topoisomerase I and II inhibitor. DACA can be used in the research of colorectal cancer, leukemia and lung cancer^[1]^[2]^[3]^[4].

IC₅₀ & Target^[1]^[2]^[3]^[4]

Topoisomerase I

Topoisomerase II

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.51 μM Compound: DACA	The compound was tested for cytotoxic activity against A2780 cell line(human ovarian carcinoma ) The compound was tested for cytotoxic activity against A2780 cell line(human ovarian carcinoma )	[PMID: 11123989]
A2780cisR	IC₅₀	0.57 μM Compound: DACA	The compound was tested for cytotoxic activity against A2780cisR cell line(human ovarian carcinoma ) The compound was tested for cytotoxic activity against A2780cisR cell line(human ovarian carcinoma )	[PMID: 11123989]
CH1	IC₅₀	0.48 μM Compound: DACA	The compound was tested for cytotoxic activity against CH1 cell line(human ovarian carcinoma ) The compound was tested for cytotoxic activity against CH1 cell line(human ovarian carcinoma )	[PMID: 11123989]
DLD-1	IC₅₀	2.3 μM Compound: 4, DACA, NSC-601316	Cytotoxicity against human DLD1 cells by Hoechst test Cytotoxicity against human DLD1 cells by Hoechst test	[PMID: 18656367]
DLD-1	IC₅₀	3.1 μM Compound: 4, DACA, NSC-601316	Cytotoxicity against human DLD1 cells by resazurin reduction test Cytotoxicity against human DLD1 cells by resazurin reduction test	[PMID: 18656367]
DU-145	IC₅₀	2 μM Compound: 8b; DACA	Antiproliferative activity against human DU-145 cells incubated for 48 hrs by Sulforhodamine B staining method Antiproliferative activity against human DU-145 cells incubated for 48 hrs by Sulforhodamine B staining method	[PMID: 33077264]
DU-145	IC₅₀	2.3 μM Compound: DACA	Antiproliferative activity against human DU145 prostate cell line Antiproliferative activity against human DU145 prostate cell line	[PMID: 10498216]
Fibroblast	IC₅₀	4.4 μM Compound: 4, DACA, NSC-601316	Cytotoxicity against human fibroblast cells by resazurin reduction test Cytotoxicity against human fibroblast cells by resazurin reduction test	[PMID: 18656367]
Fibroblast	IC₅₀	7.1 μM Compound: 4, DACA, NSC-601316	Cytotoxicity against human fibroblast cells by Hoechst test Cytotoxicity against human fibroblast cells by Hoechst test	[PMID: 18656367]
HT-29	IC₅₀	0.99 μM Compound: DACA	The compound was tested for cytotoxic activity against HT-29 cell line(human colon adeno carcinoma) The compound was tested for cytotoxic activity against HT-29 cell line(human colon adeno carcinoma)	[PMID: 11123989]
HT-29	IC₅₀	990 nM Compound: 3a	Cytotoxicity against human HT-29 cells after 144 hrs Cytotoxicity against human HT-29 cells after 144 hrs	[PMID: 18774722]
HT-29	IC₅₀	> 10 μM Compound: DACA	Antiproliferative activity against human HT-29 colon cell line Antiproliferative activity against human HT-29 colon cell line	[PMID: 10498216]
Jurkat	IC₅₀	0.3 μM Compound: 4, DACA, NSC-601316	Cytotoxicity against human Jurkat cells by Hoechst test Cytotoxicity against human Jurkat cells by Hoechst test	[PMID: 18656367]
Jurkat	IC₅₀	0.56 μM Compound: 4, DACA, NSC-601316	Cytotoxicity against human Jurkat cells by resazurin reduction test Cytotoxicity against human Jurkat cells by resazurin reduction test	[PMID: 18656367]
Jurkat	IC₅₀	580 nM Compound: 3 (DACA)	Growth inhibitory activity against human Jurkat leukemia cell line (JLC) Growth inhibitory activity against human Jurkat leukemia cell line (JLC)	[PMID: 12620081]
Jurkat	IC₅₀	580 nM Compound: 3a	Inhibitory concentration required to reduce human Jurkat leukemia (JLC sensitive, wild type) cell number to 50% of control cultures Inhibitory concentration required to reduce human Jurkat leukemia (JLC sensitive, wild type) cell number to 50% of control cultures	[PMID: 9191970]
Jurkat	IC₅₀	580 nM Compound: 8	Concentration required to inhibit 50% growth of human Jurkat cells Concentration required to inhibit 50% growth of human Jurkat cells	[PMID: 10395479]
L1210	IC₅₀	105 nM Compound: 2	Compound concentration that reduces cell growth of L1210 leukemia cultures to 50% of controls after 70h. Compound concentration that reduces cell growth of L1210 leukemia cultures to 50% of controls after 70h.	[PMID: 3361574]
L1210	IC₅₀	17000 nM Compound: 3a	Concentration required to inhibit growth of murine leukemia (L1210) cells in culture Concentration required to inhibit growth of murine leukemia (L1210) cells in culture	[PMID: 3351846]
L1210	IC₅₀	98 nM Compound: 2b	Concentration required to inhibit growth of murine leukemia (L1210) cells in culture Concentration required to inhibit growth of murine leukemia (L1210) cells in culture	[PMID: 3351846]
L1210	IC₅₀	98 nM Compound: 3	Inhibition of L1210 cell growth by 50% Inhibition of L1210 cell growth by 50%	[PMID: 11831901]
MCF7	IC₅₀	3.8 μM Compound: DACA	Antiproliferative activity against human MCF-7 breast cell line Antiproliferative activity against human MCF-7 breast cell line	[PMID: 10498216]
P388	IC₅₀	0.11 μM Compound: 1	Inhibition of P388 leukemia cells growth in culture Inhibition of P388 leukemia cells growth in culture	[PMID: 8126699]
P388	IC₅₀	0.15 μM Compound: 4	In vitro cell growth inhibitory activity against wild type P388 murine leukemia cell line (P388/W) In vitro cell growth inhibitory activity against wild type P388 murine leukemia cell line (P388/W)	[PMID: 2153829]
P388	IC₅₀	2.02 μM Compound: 4	In vitro cell growth inhibitory activity against amsacrine-resistant P388 cell line (P388/A) In vitro cell growth inhibitory activity against amsacrine-resistant P388 cell line (P388/A)	[PMID: 2153829]
P388	IC₅₀	71 nM Compound: 3 (DACA)	Growth inhibitory activity against murine P388 leukemia cells Growth inhibitory activity against murine P388 leukemia cells	[PMID: 12620081]
P388	IC₅₀	98 nM Compound: 3a	Inhibitory concentration required to reduce murine p388 leukemia cell number to 50% of control cultures Inhibitory concentration required to reduce murine p388 leukemia cell number to 50% of control cultures	[PMID: 9191970]
P388	IC₅₀	98 nM Compound: 8	Inhibitory activity against Murine p38 leukemia Inhibitory activity against Murine p38 leukemia	[PMID: 10395479]
PC-3	IC₅₀	1.86 μM Compound: 8b; DACA	Antiproliferative activity against human PC-3 cells incubated for 48 hrs by Sulforhodamine B staining method Antiproliferative activity against human PC-3 cells incubated for 48 hrs by Sulforhodamine B staining method	[PMID: 33077264]
SK-OV-3	IC₅₀	0.98 μM Compound: DACA	The compound was tested for cytotoxic activity against SKOV-3 cell line(human ovarian carcinoma ) The compound was tested for cytotoxic activity against SKOV-3 cell line(human ovarian carcinoma )	[PMID: 11123989]
SK-OV-3	IC₅₀	2.4 μM Compound: DACA	Antiproliferative activity against human SKOV-3 ovarian cell line Antiproliferative activity against human SKOV-3 ovarian cell line	[PMID: 10498216]

In Vitro

DACA (0.1-100 μM; 2 h) stabilizes topoisomerase II cleavable complexes in a dose-dependent manner in human leukaemia CCRF-CEM cells, forms topoisomerase IIβ cleavable complexes only at the highest concentration of 100 μM^[1].
DACA exhibits a pattern of activity distinct from that of Amsacrine (HY-13551) and Etoposide (HY-13629) against a variety of human and mouse cell lines, including primary human melanoma cultures derived from fresh surgical melanoma specimens, with IC₅₀ values ranging from 0.09 μM to 3.4 μM^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

DACA is highly active against Lewis lung carcinoma in mice^[4].
Studies have shown that DACA has significant potential for clinical application. First, DACA can overcome drug resistance in various types of cancer cells. Second, DACA exhibits high activity against certain solid tumor models in vitro and in vivo. Third, DACA appears to be able to cross the blood-brain barrier in animal models. Finally, DACA exhibits linear pharmacokinetic characteristics in preclinical models^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

293.36

Formula

C₁₈H₁₉N₃O

CAS No.

89459-25-6

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC=CC2=CC3=CC=CC=C3N=C12)NCCN(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (340.88 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4088 mL	17.0439 mL	34.0878 mL
5 mM	0.6818 mL	3.4088 mL	6.8176 mL
10 mM	0.3409 mL	1.7044 mL	3.4088 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.89%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (247 KB) HNMR (237 KB) LCMS (117 KB)

Handling Instructions (2659 KB)

References

[1]. Padget K, et al. An investigation into the formation of N- [2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and 6-[2-(dimethylamino)ethylamino]- 3-hydroxy-7H-indeno[2, 1-C]quinolin-7-one dihydrochloride (TAS-103) stabilised DNA topoisomerase I and II cleavable complexes in human leukaemia cells. Biochem Pharmacol. 2000;60(6):817-821. [Content Brief]

[2]. Dittrich C, et al. Phase II study of XR 5000 (DACA), an inhibitor of topoisomerase I and II, administered as a 120-h infusion in patients with non-small cell lung cancer. Eur J Cancer. 2003 Feb;39(3):330-4. [Content Brief]

[3]. Caponigro F, et al. Phase II study of XR 5000, an inhibitor of topoisomerases I and II, in advanced colorectal cancer. Eur J Cancer. 2002 Jan;38(1):70-4. [Content Brief]

[4]. Twelves CJ, et al. Phase I and pharmacokinetic study of DACA (XR5000): a novel inhibitor of topoisomerase I and II. CRC Phase I/II Committee. Br J Cancer. 1999 Aug;80(11):1786-91. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4088 mL	17.0439 mL	34.0878 mL	85.2195 mL
	5 mM	0.6818 mL	3.4088 mL	6.8176 mL	17.0439 mL
	10 mM	0.3409 mL	1.7044 mL	3.4088 mL	8.5220 mL
	15 mM	0.2273 mL	1.1363 mL	2.2725 mL	5.6813 mL
	20 mM	0.1704 mL	0.8522 mL	1.7044 mL	4.2610 mL
	25 mM	0.1364 mL	0.6818 mL	1.3635 mL	3.4088 mL
	30 mM	0.1136 mL	0.5681 mL	1.1363 mL	2.8407 mL
	40 mM	0.0852 mL	0.4261 mL	0.8522 mL	2.1305 mL
	50 mM	0.0682 mL	0.3409 mL	0.6818 mL	1.7044 mL
	60 mM	0.0568 mL	0.2841 mL	0.5681 mL	1.4203 mL
	80 mM	0.0426 mL	0.2130 mL	0.4261 mL	1.0652 mL
	100 mM	0.0341 mL	0.1704 mL	0.3409 mL	0.8522 mL

DACA Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DACA89459-25-6Topoisomerasehuman leukaemia CCRF-CEM cellsDNA topoisomerase I and II cleavable complexesInhibitorinhibitorinhibit

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DACA

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DACA Related Antibodies

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Complete Stock Solution Preparation Table

DACA Related Classifications

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