Tasquinimod | ABR-215050 | S100A9 Inhibitor | AmBeed-信号通路专用抑制剂

Tasquinimod/他喹莫德 {[allProObj[0].p_purity_real_show]}

货号：A337216 同义名： ABR-215050

Tasquinimod是一种通过全酶抑制HDAC4信号通路的别构抑制剂，具有抗血管生成和抗肿瘤作用。它是奎啶-3-羧酰胺类化合物。

Tasquinimod/他喹莫德化学结构
CAS号：254964-60-8

Tasquinimod/他喹莫德 3D分子结构
CAS号：254964-60-8

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组蛋白去乙酰化酶亚型比较

产品名称	HD1 ↓ ↑	HD2 ↓ ↑	HDAC ↓ ↑	HDAC1 ↓ ↑	HDAC10 ↓ ↑	HDAC11 ↓ ↑	HDAC2 ↓ ↑	HDAC3 ↓ ↑	HDAC4 ↓ ↑	HDAC5 ↓ ↑	HDAC6 ↓ ↑	HDAC7 ↓ ↑	HDAC8 ↓ ↑	HDAC9 ↓ ↑	其他靶点	纯度
Givinostat HCl monohydrate	++++ HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-A (Maize), IC50: 100 nM HD1-B (Maize), IC50: 3.4 μM															96%
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													99%+
Scriptaid			✔													99%+
Valproic acid sodium			✔												Autophagy	97%
AR-42			+++ HDAC, IC50: 30 nM													99%+
Dacinostat			+++ HDAC, IC50: 32 nM													98+%
CUDC-101			++++ HDAC, IC50: 4.4 nM	++++ HDAC1, IC50: 4.5 nM	+++ HDAC10, IC50: 26.1 nM		+++ HDAC2, IC50: 12.6 nM	++++ HDAC3, IC50: 9.1 nM	+++ HDAC4, IC50: 13.2 nM	+++ HDAC5, IC50: 11.4 nM	++++ HDAC6, IC50: 5.1 nM	+ HDAC7, IC50: 373 nM	++ HDAC8, IC50: 79.8 nM	++ HDAC9, IC50: 67.2 nM	HER2,EGFR	99%+
M344			++ HDAC, IC50: 100 nM													99%+
Splitomicin			+ Sir2p, IC50: 60 μM													99%
Panobinostat			++++ HDAC (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												Nrf2,NF-κB	98%
Belinostat			+++ HDAC, IC50: 27 nM													98%
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								98%
Valproic acid				+ HDAC1, IC50: 0.4 mM												98%
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								99%+
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								98%
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					98+%
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									99%+
Parthenolide				✔											p53,NF-κB	97% HPLC
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								98%
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								98%
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					99%+
Fimepinostat				++++ HDAC1, IC50: 1.7 nM	++++ HDAC10, IC50: 2.8 nM	++++ HDAC11, IC50: 5.4 nM	++++ HDAC2, IC50: 5.0 nM	++++ HDAC3, IC50: 1.8 nM			+++ HDAC6, IC50: 27 nM					99%+
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								99%+
Santacruzamate A							++++ HDAC2, IC50: 119 pM									99%+
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								99%+
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						99%+
Tasquinimod									✔							99%+
CAY10603											++++ HDAC6, IC50: 2 pM					98%
Tubastatin A											+++ HDAC6, IC50: 15 nM					98%
Tubacin											++++ HDAC6, IC50: 4 nM					99%+
ACY-738											++++ HDAC6, IC50: 1.7 nM					99%+
Nexturastat A											++++ HDAC6, IC50: 5 nM					99%+
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			99%
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			98%
PCI-34051													+++ HDAC8, IC50: 10 nM			99%+
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			99%+
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			99%+
Abexinostat				++++ HDAC1, Ki: 7 nM	+++ HDAC10, IC50: 24 nM		+++ HDAC2, Ki: 19 nM	++++ HDAC3/SMRT, Ki: 8.2 nM			+++ HDAC6, Ki: 17 nM		+ HDAC8, IC50: 280 nM			98%+
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			99%+
HPOB				+ HDAC1, IC50: 2.9 μM	+ HDAC10, IC50: 3.0 μM		+ HDAC2, IC50: 4.4 μM	+ HDAC3, IC50: 1.7 μM			++ HDAC6, IC50: 56 nM		+ HDAC8, IC50: 2.8 μM			97%
Quisinostat 2HCl				++++ HDAC1, IC50: 0.11 nM	++++ HDAC10, IC50: 0.46 nM	++++ HDAC11, IC50: 0.37 nM	++++ HDAC2, IC50: 0.33 nM	++++ HDAC3, IC50: 4.86 nM	++++ HDAC4, IC50: 0.64 nM	++++ HDAC5, IC50: 3.69 nM			++++ HDAC8, IC50: 4.26 nM			97%
Domatinostat				+ HDAC1, IC50: 1.20 μM	+ HDAC10, IC50: 21 μM	+ HDAC11, IC50: 9.7 μM	+ HDAC2, IC50: 1.12 μM	+ HDAC3, IC50: 0.57 μM		+ HDAC5, IC50: 11.3 μM				+ HDAC9, IC50: 50 μM		99%+
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		99%+
Pracinostat				++ HDAC1, IC50: 49 nM	+++ HDAC10, IC50: 40 nM	++ HDAC11, IC50: 93 nM	++ HDAC2, IC50: 96 nM	+++ HDAC3, IC50: 43 nM	++ HDAC4, IC50: 56 nM	+++ HDAC5, IC50: 47 nM	+ HDAC6, IC50: 1.008 μM	++ HDAC7, IC50: 137 nM	++ HDAC8, IC50: 140 nM	++ HDAC9, IC50: 70 nM		99%+
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tasquinimod/他喹莫德生物活性

靶点

HDAC4

描述

Tasquinimod is a novel inhibitor of tumor angiogenesis that enhances the therapeutic anticancer response when combine with other standard-of-care modalities (radiation, androgen ablation, and/or taxan-based chemotherapies) in experimental animal models^[3]. Tasquinimod has been documented to have a robust and consistent anti-angiogenic activity in vitro at dose between 10-50μM and in vivo at 1-10mg/kg/day resulting in a potent anti-tumor effect in rodent and human prostate cancer xenografts tested in the same dose range^[4].

Tasquinimod/他喹莫德细胞实验

Cell Line LNCaP cells LP-1 OPM-2 RPMI-8226 5TGM1 KG-1a cells MOLM-13 cells MCF-10A/ErbB2* cells Nasopharyngeal carcinoma cells LNCaP cells LNCaP19 cells MC38-C215 cells HUVECs LNCaP cells	Concentration	Treated Time	Description	References
LNCaP cells	50 µM	24 hours	To investigate the effect of Tasquinimod on gene expression, results showed significant up-regulation of TSP1 gene.	Mol Cancer. 2010 May 17;9:107.
LP-1	10 µM and 25 µM	24 hours, 48 hours, 72 hours and 120 hours	Tasquinimod significantly decreased myeloma cell proliferation and colony formation in vitro, associated with an inhibition of c- MYC and increased p27 expression.	J Immunother Cancer. 2023 Jan;11(1):e005319.
OPM-2	10 µM and 25 µM	24 hours, 48 hours, 72 hours and 120 hours	Tasquinimod significantly decreased myeloma cell proliferation and colony formation in vitro, associated with an inhibition of c- MYC and increased p27 expression.	J Immunother Cancer. 2023 Jan;11(1):e005319.
RPMI-8226	10 µM and 25 µM	24 hours, 48 hours, 72 hours and 120 hours	Tasquinimod significantly decreased myeloma cell proliferation and colony formation in vitro, associated with an inhibition of c- MYC and increased p27 expression.	J Immunother Cancer. 2023 Jan;11(1):e005319.
5TGM1	10 µM and 25 µM	24 hours, 48 hours, 72 hours and 120 hours	Tasquinimod significantly decreased myeloma cell proliferation and colony formation in vitro, associated with an inhibition of c- MYC and increased p27 expression.	J Immunother Cancer. 2023 Jan;11(1):e005319.
KG-1a cells	10, 25 µM	24, 48 hours	To evaluate the effect of tasquinimod on AML cell survival and proliferation, results showed that tasquinimod significantly reduced AML cell viability and proliferation, and increased apoptosis.	Blood Cancer J. 2023 Dec 18;13(1):188.
MOLM-13 cells	10, 25 µM	24, 48 hours	To evaluate the effect of tasquinimod on AML cell survival and proliferation, results showed that tasquinimod significantly reduced AML cell viability and proliferation, and increased apoptosis.	Blood Cancer J. 2023 Dec 18;13(1):188.
MCF-10A/ErbB2* cells	10 µM	48 hours	To study the effect of Tasquinimod on S100A8/9 expression, results showed that Tasquinimod significantly inhibited the expression of S100A8/9.	Genes Dev. 2015 Aug 1;29(15):1631-48.
Nasopharyngeal carcinoma cells	5 µM	48 hours	Tasquinimod significantly impaired cell proliferation and colony formation in HDAC4-overexpressing cells, indicating that Tasquinimod suppresses nasopharyngeal carcinoma cell proliferation by inhibiting HDAC4 activity.	Cell Death Dis. 2021 Feb 1;12(2):137.
LNCaP cells	10 µM	72 hours	To investigate the effect of Tasquinimod on TSP1 mRNA expression, results showed significant up-regulation of TSP1 mRNA after 72 hours.	Mol Cancer. 2010 May 17;9:107.
LNCaP19 cells	10 µM	72 hours	To investigate the effect of Tasquinimod on TSP1 mRNA expression, results showed up-regulation of TSP1 mRNA in LNCaP19 cells.	Mol Cancer. 2010 May 17;9:107.
MC38-C215 cells	1 –10 µM	72 hours	To evaluate the effect of Tasquinimod on the proliferation of MC38-C215 cells, results showed that Tasquinimod did not significantly inhibit cell proliferation under normoxic or hypoxic conditions.	J Immunother Cancer. 2015 Dec 15;3:53.
HUVECs	1 µM	one week	Tasquinimod inhibits the growth of HUVECs under stressful conditions	Cancer Res. 2013 Feb 15;73(4):1386-99.
LNCaP cells	1 µM	one week	Tasquinimod induces cell death in LNCaP cells under stressful conditions	Cancer Res. 2013 Feb 15;73(4):1386-99.

Cell Line

Concentration

Treated Time

Description

References

LNCaP cells

50 µM

24 hours

To investigate the effect of Tasquinimod on gene expression, results showed significant up-regulation of TSP1 gene.

Mol Cancer. 2010 May 17;9:107.

LP-1

10 µM and 25 µM

24 hours, 48 hours, 72 hours and 120 hours

Tasquinimod significantly decreased myeloma cell proliferation and colony formation in vitro, associated with an inhibition of c- MYC and increased p27 expression.

J Immunother Cancer. 2023 Jan;11(1):e005319.

OPM-2

10 µM and 25 µM

24 hours, 48 hours, 72 hours and 120 hours

Tasquinimod significantly decreased myeloma cell proliferation and colony formation in vitro, associated with an inhibition of c- MYC and increased p27 expression.

J Immunother Cancer. 2023 Jan;11(1):e005319.

RPMI-8226

10 µM and 25 µM

24 hours, 48 hours, 72 hours and 120 hours

Tasquinimod significantly decreased myeloma cell proliferation and colony formation in vitro, associated with an inhibition of c- MYC and increased p27 expression.

J Immunother Cancer. 2023 Jan;11(1):e005319.

5TGM1

10 µM and 25 µM

24 hours, 48 hours, 72 hours and 120 hours

Tasquinimod significantly decreased myeloma cell proliferation and colony formation in vitro, associated with an inhibition of c- MYC and increased p27 expression.

J Immunother Cancer. 2023 Jan;11(1):e005319.

KG-1a cells

10, 25 µM

24, 48 hours

To evaluate the effect of tasquinimod on AML cell survival and proliferation, results showed that tasquinimod significantly reduced AML cell viability and proliferation, and increased apoptosis.

Blood Cancer J. 2023 Dec 18;13(1):188.

MOLM-13 cells

10, 25 µM

24, 48 hours

To evaluate the effect of tasquinimod on AML cell survival and proliferation, results showed that tasquinimod significantly reduced AML cell viability and proliferation, and increased apoptosis.

Blood Cancer J. 2023 Dec 18;13(1):188.

MCF-10A/ErbB2* cells

10 µM

48 hours

To study the effect of Tasquinimod on S100A8/9 expression, results showed that Tasquinimod significantly inhibited the expression of S100A8/9.

Genes Dev. 2015 Aug 1;29(15):1631-48.

Nasopharyngeal carcinoma cells

5 µM

48 hours

Tasquinimod significantly impaired cell proliferation and colony formation in HDAC4-overexpressing cells, indicating that Tasquinimod suppresses nasopharyngeal carcinoma cell proliferation by inhibiting HDAC4 activity.

Cell Death Dis. 2021 Feb 1;12(2):137.

LNCaP cells

10 µM

72 hours

To investigate the effect of Tasquinimod on TSP1 mRNA expression, results showed significant up-regulation of TSP1 mRNA after 72 hours.

Mol Cancer. 2010 May 17;9:107.

LNCaP19 cells

10 µM

72 hours

To investigate the effect of Tasquinimod on TSP1 mRNA expression, results showed up-regulation of TSP1 mRNA in LNCaP19 cells.

Mol Cancer. 2010 May 17;9:107.

MC38-C215 cells

1 –10 µM

72 hours

To evaluate the effect of Tasquinimod on the proliferation of MC38-C215 cells, results showed that Tasquinimod did not significantly inhibit cell proliferation under normoxic or hypoxic conditions.

J Immunother Cancer. 2015 Dec 15;3:53.

HUVECs

1 µM

one week

Tasquinimod inhibits the growth of HUVECs under stressful conditions

Cancer Res. 2013 Feb 15;73(4):1386-99.

LNCaP cells

1 µM

one week

Tasquinimod induces cell death in LNCaP cells under stressful conditions

Cancer Res. 2013 Feb 15;73(4):1386-99.

Tasquinimod/他喹莫德动物实验

Species Mice Mice Nude mice Mice BABL/C mice Nude mice Nude mice FVB mice Rats C57Bl/6 mice C57BL/KaLwRij mice C57BL/6 mice	Animal Model MBT-2 mouse model NOD scid mice Nasopharyngeal carcinoma subcutaneous xenograft model Tuberculosis infection model DSS-induced ulcerative colitis model LNCaP prostate tumor model CWR22-RH human prostate cancer xenograft model Castration-resistant prostate cancer model AY-27 rat model MC38-C215 colon carcinoma model 5TGM1 and 5T33MM models MC38 colon cancer model	Administration	Dosage	Frequency	Description	References
Mice	MBT-2 mouse model	Oral gavage	0.1, 1, 10, and 30 mg/kg	Twice daily for 21 days	Tasquinimod was effective in preventing early stage tumor growth but did not achieve a clear antitumor effect in advanced tumors. The combination of tasquinimod with an Anti-PD-L1 antibody enhanced the antitumor immune response in bladder tumors.	Oncoimmunology. 2016 Feb 18;5(6):e1145333
Mice	NOD scid mice	Oral	10 mg/kg	Once daily for 4 days	To study the effect of Tasquinimod on the growth of HR?/HER2+ breast cancer tumors, results showed that Tasquinimod significantly reduced tumor growth.	Genes Dev. 2015 Aug 1;29(15):1631-48.
Nude mice	Nasopharyngeal carcinoma subcutaneous xenograft model	Intragastric administration	10 mg/kg	Every 3 days for 5 weeks	Tasquinimod significantly inhibited tumor growth in HDAC4-overexpressing cells, indicating that Tasquinimod suppresses nasopharyngeal carcinoma tumor growth by inhibiting HDAC4 activity.	Cell Death Dis. 2021 Feb 1;12(2):137.
Mice	Tuberculosis infection model	Oral	10 mg/kg	Once daily, 7 days/week	Tasquinimod monotherapy enhances bacterial clearance in a mouse model of tuberculosis infection, reduces bacterial burden in lungs and spleens, and significantly decreases the frequency of regulatory T cells (Tregs) and myeloid-derived suppressor cells (MDSCs).	Am J Respir Crit Care Med. 2019 Feb 1;199(3):386-389
BABL/C mice	DSS-induced ulcerative colitis model	Oral	10 mg/kg	Administered on days 1, 3, and 5, lasting for 7 days	To evaluate the therapeutic effect of MM-PLGA-TAS on DSS-induced ulcerative colitis, the results showed that MM-PLGA-TAS significantly improved weight loss and disease activity index (DAI) scores in mice, and reduced colonic inflammation.	J Innate Immun. 2022;14(4):380-392
Nude mice	LNCaP prostate tumor model	Oral	10 mg/kg/day	Once daily for 3 weeks	To investigate the effect of Tasquinimod on tumor growth, results showed significant inhibition of tumor growth and up-regulation of TSP1 mRNA and protein levels.	Mol Cancer. 2010 May 17;9:107.
Nude mice	CWR22-RH human prostate cancer xenograft model	Oral	10 mg/kg/day	Daily administration until tumor growth reaches 0.250cc	Tasquinimod inhibits tumor growth under tumor microenvironment stress	Cancer Res. 2013 Feb 15;73(4):1386-99.
FVB mice	Castration-resistant prostate cancer model	Drinking water	10 mg/kg/day	Daily, for 3-4 weeks	Tasquinimod significantly enhanced the antitumor effects of two different immunotherapeutics and inhibited distinct MDSC populations and M2-polarized TAMs.	Cancer Immunol Res. 2015 Feb;3(2):136-48
Rats	AY-27 rat model	Oral gavage	2 mg/kg	28 days	Tasquinimod was effective in preventing early stage tumor growth but did not achieve a clear antitumor effect in advanced tumors. The combination of tasquinimod with an Anti-PD-L1 antibody enhanced the antitumor immune response in bladder tumors.	Oncoimmunology. 2016 Feb 18;5(6):e1145333
C57Bl/6 mice	MC38-C215 colon carcinoma model	Oral	30 mg/kg	Daily, for 14 days	To evaluate the effect of Tasquinimod on the growth of MC38-C215 tumors, results showed that Tasquinimod significantly inhibited tumor growth, reduced the number of M2 macrophages in the tumor, and increased the number of M1 macrophages.	J Immunother Cancer. 2015 Dec 15;3:53.
C57BL/KaLwRij mice	5TGM1 and 5T33MM models	Oral	30 mg/kg	Daily until the end of the experiment	Tasquinimod significantly reduced the tumor load and increased the trabecular bone volume, which resulted in prolonged overall survival of MM- bearing mice in vivo.	J Immunother Cancer. 2023 Jan;11(1):e005319.
C57BL/6 mice	MC38 colon cancer model	Oral gavage	30 mg/kg	Once daily for 15 days	To evaluate the antitumor efficacy of Tasquinimod in combination with anti-PD-1 antibody in the MC38 colon cancer model. The results showed that the combination treatment significantly delayed tumor growth and exhibited higher tumor inhibition efficacy compared to anti-PD-1 or Tasquinimod alone.	Cell Rep Med. 2023 Apr 18;4(4):100987

Species

Animal Model

Administration

Dosage

Frequency

Description

References

Mice

MBT-2 mouse model

Oral gavage

0.1, 1, 10, and 30 mg/kg

Twice daily for 21 days

Tasquinimod was effective in preventing early stage tumor growth but did not achieve a clear antitumor effect in advanced tumors. The combination of tasquinimod with an Anti-PD-L1 antibody enhanced the antitumor immune response in bladder tumors.

Oncoimmunology. 2016 Feb 18;5(6):e1145333

Mice

NOD scid mice

Oral

10 mg/kg

Once daily for 4 days

To study the effect of Tasquinimod on the growth of HR?/HER2+ breast cancer tumors, results showed that Tasquinimod significantly reduced tumor growth.

Genes Dev. 2015 Aug 1;29(15):1631-48.

Nude mice

Nasopharyngeal carcinoma subcutaneous xenograft model

Intragastric administration

10 mg/kg

Every 3 days for 5 weeks

Tasquinimod significantly inhibited tumor growth in HDAC4-overexpressing cells, indicating that Tasquinimod suppresses nasopharyngeal carcinoma tumor growth by inhibiting HDAC4 activity.

Cell Death Dis. 2021 Feb 1;12(2):137.

Mice

Tuberculosis infection model

Oral

10 mg/kg

Once daily, 7 days/week

Tasquinimod monotherapy enhances bacterial clearance in a mouse model of tuberculosis infection, reduces bacterial burden in lungs and spleens, and significantly decreases the frequency of regulatory T cells (Tregs) and myeloid-derived suppressor cells (MDSCs).

Am J Respir Crit Care Med. 2019 Feb 1;199(3):386-389

BABL/C mice

DSS-induced ulcerative colitis model

Oral

10 mg/kg

Administered on days 1, 3, and 5, lasting for 7 days

To evaluate the therapeutic effect of MM-PLGA-TAS on DSS-induced ulcerative colitis, the results showed that MM-PLGA-TAS significantly improved weight loss and disease activity index (DAI) scores in mice, and reduced colonic inflammation.

J Innate Immun. 2022;14(4):380-392

Nude mice

LNCaP prostate tumor model

Oral

10 mg/kg/day

Once daily for 3 weeks

To investigate the effect of Tasquinimod on tumor growth, results showed significant inhibition of tumor growth and up-regulation of TSP1 mRNA and protein levels.

Mol Cancer. 2010 May 17;9:107.

Nude mice

CWR22-RH human prostate cancer xenograft model

Oral

10 mg/kg/day

Daily administration until tumor growth reaches 0.250cc

Tasquinimod inhibits tumor growth under tumor microenvironment stress

Cancer Res. 2013 Feb 15;73(4):1386-99.

FVB mice

Castration-resistant prostate cancer model

Drinking water

10 mg/kg/day

Daily, for 3-4 weeks

Tasquinimod significantly enhanced the antitumor effects of two different immunotherapeutics and inhibited distinct MDSC populations and M2-polarized TAMs.

Cancer Immunol Res. 2015 Feb;3(2):136-48

Rats

AY-27 rat model

Oral gavage

2 mg/kg

28 days

Oncoimmunology. 2016 Feb 18;5(6):e1145333

C57Bl/6 mice

MC38-C215 colon carcinoma model

Oral

30 mg/kg

Daily, for 14 days

To evaluate the effect of Tasquinimod on the growth of MC38-C215 tumors, results showed that Tasquinimod significantly inhibited tumor growth, reduced the number of M2 macrophages in the tumor, and increased the number of M1 macrophages.

J Immunother Cancer. 2015 Dec 15;3:53.

C57BL/KaLwRij mice

5TGM1 and 5T33MM models

Oral

30 mg/kg

Daily until the end of the experiment

Tasquinimod significantly reduced the tumor load and increased the trabecular bone volume, which resulted in prolonged overall survival of MM- bearing mice in vivo.

J Immunother Cancer. 2023 Jan;11(1):e005319.

C57BL/6 mice

MC38 colon cancer model

Oral gavage

30 mg/kg

Once daily for 15 days

To evaluate the antitumor efficacy of Tasquinimod in combination with anti-PD-1 antibody in the MC38 colon cancer model. The results showed that the combination treatment significantly delayed tumor growth and exhibited higher tumor inhibition efficacy compared to anti-PD-1 or Tasquinimod alone.

Cell Rep Med. 2023 Apr 18;4(4):100987

Tasquinimod/他喹莫德参考文献

Tasquinimod/他喹莫德实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.61mL

4.92mL

2.46mL

Tasquinimod/他喹莫德技术信息

CAS号	254964-60-8
分子式	C₂₀H₁₇F₃N₂O₄
分子量	406.36
SMILES Code	O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2OC)N(C)C3=CC=C(C(F)(F)F)C=C3
MDL No.	MFCD18251454

别名	ABR-215050
运输	蓝冰
InChI Key	ONDYALNGTUAJDX-UHFFFAOYSA-N
Pubchem ID	54682876

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 40 mg/mL(98.44 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

方案四

方案五

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