Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer[1][2][3].
IC50 & Target[1]
RARα
2.4 nM (Ki)
RARβ
400 nM (Ki)
体外研究 (In Vitro)
Amsilarotene (0, 10, 25 μM; 24 hours) induces apoptosis of human epithelial ovarian carcinoma-derived cell lines in a concentration-dependent manner[2]. Amsilarotene (10, 20 μM; 0, 3, 6, and 9 days) inhibits the proliferation of BxPC-3 and MIAPaCa-2 cells[3]. Amsilarotene (10 μM; 48 hours) increases the proportion of sensitive BxPC-3 cells in the G1 phase[3]. Amsilarotene (10 μM; 0, 3, 6, 24, 48, 72 hours) inhibits the retinoblastoma-gene product (RB) phosphorylation in BxPC-3 cells between 24 and 72 hours[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis[2]
Cell Line:
RMG-I, RMG-II, RTSG, RMUG-S, RMUG-L, and KF cells
Concentration:
0, 10, 25 μM
Incubation Time:
24 hours
Result:
Induced apoptosis in a concentration-dependent manner in all of the cell lines, except KF cells.
Cell Proliferation Assay[3]
Cell Line:
BxPC-3, MIAPaCa-2, AsPC-1 cells
Concentration:
10 and 20 μM
Incubation Time:
0, 3, 6, and 9 days.
Result:
Inhibited the proliferation of BxPC-3 and MIAPaCa-2 cells, but not the proliferation of AsPC-1 cells.
Cell Cycle Analysis[3]
Cell Line:
Sensitive BxPC-3 cells
Concentration:
10 μM
Incubation Time:
48 hours
Result:
The proportion of cells in the G1 phase increased from 43% of untreated control cells to 86%
体内研究 (In Vivo)
Amsilarotene (8 mg/kg/day orally for 30 days) inhibits the RMG-II tumor growth in nude mice[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
6-week-old female BALB/c nu/nu mice with subcutaneous RMG-II tumors[2]
Dosage:
8 mg/kg/day
Administration:
Orally for 30 days
Result:
The maximal tumor growth-inhibiting effect was seen on day 31 of administration, when there was a 45% reduction of relative tumor volume (RTV).
分子量
385.60
Formula
C20H27NO3Si2
CAS 号
125973-56-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Sun SY, et al. Differential effects of synthetic nuclear retinoid receptor-selective retinoids on the growth of human non-small cell lung carcinoma cells. Cancer Res. 1997 Nov 1;57(21):4931-9.
[2]. Suzuki N, et al. A novel retinoid, 4-[3,5-bis (trimethylsilyl) benzamido] benzoic acid (TAC-101), induces apoptosis of human ovarian carcinoma cells and shows potential as a new antitumor agent for clear cell adenocarcinoma. Gynecol Oncol. 2004 Sep;94(3):643-9.
[3]. Fujimoto K, et al. Induction of cell-cycle arrest and apoptosis by a novel retinobenzoic-acid derivative, TAC-101, in human pancreatic-cancer cells. Int J Cancer. 1999 May 17;81(4):637-44.
Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer[1][2][3].
IC50 & Target[1]
RARα
2.4 nM (Ki)
RARβ
400 nM (Ki)
体外研究 (In Vitro)
Amsilarotene (0, 10, 25 μM; 24 hours) induces apoptosis of human epithelial ovarian carcinoma-derived cell lines in a concentration-dependent manner[2]. Amsilarotene (10, 20 μM; 0, 3, 6, and 9 days) inhibits the proliferation of BxPC-3 and MIAPaCa-2 cells[3]. Amsilarotene (10 μM; 48 hours) increases the proportion of sensitive BxPC-3 cells in the G1 phase[3]. Amsilarotene (10 μM; 0, 3, 6, 24, 48, 72 hours) inhibits the retinoblastoma-gene product (RB) phosphorylation in BxPC-3 cells between 24 and 72 hours[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis[2]
Cell Line:
RMG-I, RMG-II, RTSG, RMUG-S, RMUG-L, and KF cells
Concentration:
0, 10, 25 μM
Incubation Time:
24 hours
Result:
Induced apoptosis in a concentration-dependent manner in all of the cell lines, except KF cells.
Cell Proliferation Assay[3]
Cell Line:
BxPC-3, MIAPaCa-2, AsPC-1 cells
Concentration:
10 and 20 μM
Incubation Time:
0, 3, 6, and 9 days.
Result:
Inhibited the proliferation of BxPC-3 and MIAPaCa-2 cells, but not the proliferation of AsPC-1 cells.
Cell Cycle Analysis[3]
Cell Line:
Sensitive BxPC-3 cells
Concentration:
10 μM
Incubation Time:
48 hours
Result:
The proportion of cells in the G1 phase increased from 43% of untreated control cells to 86%
体内研究 (In Vivo)
Amsilarotene (8 mg/kg/day orally for 30 days) inhibits the RMG-II tumor growth in nude mice[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
6-week-old female BALB/c nu/nu mice with subcutaneous RMG-II tumors[2]
Dosage:
8 mg/kg/day
Administration:
Orally for 30 days
Result:
The maximal tumor growth-inhibiting effect was seen on day 31 of administration, when there was a 45% reduction of relative tumor volume (RTV).
分子量
385.60
Formula
C20H27NO3Si2
CAS 号
125973-56-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Sun SY, et al. Differential effects of synthetic nuclear retinoid receptor-selective retinoids on the growth of human non-small cell lung carcinoma cells. Cancer Res. 1997 Nov 1;57(21):4931-9.
[2]. Suzuki N, et al. A novel retinoid, 4-[3,5-bis (trimethylsilyl) benzamido] benzoic acid (TAC-101), induces apoptosis of human ovarian carcinoma cells and shows potential as a new antitumor agent for clear cell adenocarcinoma. Gynecol Oncol. 2004 Sep;94(3):643-9.
[3]. Fujimoto K, et al. Induction of cell-cycle arrest and apoptosis by a novel retinobenzoic-acid derivative, TAC-101, in human pancreatic-cancer cells. Int J Cancer. 1999 May 17;81(4):637-44.
Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer[1][2][3].
IC50 & Target[1]
RARα
2.4 nM (Ki)
RARβ
400 nM (Ki)
体外研究 (In Vitro)
Amsilarotene (0, 10, 25 μM; 24 hours) induces apoptosis of human epithelial ovarian carcinoma-derived cell lines in a concentration-dependent manner[2]. Amsilarotene (10, 20 μM; 0, 3, 6, and 9 days) inhibits the proliferation of BxPC-3 and MIAPaCa-2 cells[3]. Amsilarotene (10 μM; 48 hours) increases the proportion of sensitive BxPC-3 cells in the G1 phase[3]. Amsilarotene (10 μM; 0, 3, 6, 24, 48, 72 hours) inhibits the retinoblastoma-gene product (RB) phosphorylation in BxPC-3 cells between 24 and 72 hours[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis[2]
Cell Line:
RMG-I, RMG-II, RTSG, RMUG-S, RMUG-L, and KF cells
Concentration:
0, 10, 25 μM
Incubation Time:
24 hours
Result:
Induced apoptosis in a concentration-dependent manner in all of the cell lines, except KF cells.
Cell Proliferation Assay[3]
Cell Line:
BxPC-3, MIAPaCa-2, AsPC-1 cells
Concentration:
10 and 20 μM
Incubation Time:
0, 3, 6, and 9 days.
Result:
Inhibited the proliferation of BxPC-3 and MIAPaCa-2 cells, but not the proliferation of AsPC-1 cells.
Cell Cycle Analysis[3]
Cell Line:
Sensitive BxPC-3 cells
Concentration:
10 μM
Incubation Time:
48 hours
Result:
The proportion of cells in the G1 phase increased from 43% of untreated control cells to 86%
体内研究 (In Vivo)
Amsilarotene (8 mg/kg/day orally for 30 days) inhibits the RMG-II tumor growth in nude mice[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
6-week-old female BALB/c nu/nu mice with subcutaneous RMG-II tumors[2]
Dosage:
8 mg/kg/day
Administration:
Orally for 30 days
Result:
The maximal tumor growth-inhibiting effect was seen on day 31 of administration, when there was a 45% reduction of relative tumor volume (RTV).
分子量
385.60
Formula
C20H27NO3Si2
CAS 号
125973-56-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Sun SY, et al. Differential effects of synthetic nuclear retinoid receptor-selective retinoids on the growth of human non-small cell lung carcinoma cells. Cancer Res. 1997 Nov 1;57(21):4931-9.
[2]. Suzuki N, et al. A novel retinoid, 4-[3,5-bis (trimethylsilyl) benzamido] benzoic acid (TAC-101), induces apoptosis of human ovarian carcinoma cells and shows potential as a new antitumor agent for clear cell adenocarcinoma. Gynecol Oncol. 2004 Sep;94(3):643-9.
[3]. Fujimoto K, et al. Induction of cell-cycle arrest and apoptosis by a novel retinobenzoic-acid derivative, TAC-101, in human pancreatic-cancer cells. Int J Cancer. 1999 May 17;81(4):637-44.