TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo[1].
IC50 & Target
Antifolate, DHFR[1]
体外研究 (In Vitro)
TNP-351 inhibits the proliferation of mouse L1210 leukemia cells and human CCRF-CEM lymphoblastic leukemia cells with ED50 values of 0.79 and 2.7 nM, respectively[1]. The ED50 values determined for the parent cell line CCRF-CEM, CCRFCEM R30/6 subline, CCRF-CEM R1, and CCRF-CEM R2 are 2.7, 5.8, 94 and 76 nM, respectively[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
L1210 and CCRF-CEM cells
Concentration:
0.1, 0.3, 1, 3, and 10 nM for L1210 cells; 0.3, 1, 3, 10, and 30 for CCRF-CEM cells
Incubation Time:
48 hours for L1210 cells; 72 hours for CCRF-CEM cells
Result:
The ED50 values were 0.79 and 2.7 nM for L1210 and CCRF-CEM cells, respectively.
分子量
440.45
Formula
C21H24N6O5
CAS 号
125991-51-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. F Itoh ,et al. Novel pyrrolo[2,3-d]pyrimidine Antifolate TNP-351: Cytotoxic Effect on Methotrexate-Resistant CCRF-CEM Cells and Inhibition of Transformylases of De Novo Purine Biosynthesis. Cancer Chemother Pharmacol. 1994;34(4):273-9.
TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo[1].
IC50 & Target
Antifolate, DHFR[1]
体外研究 (In Vitro)
TNP-351 inhibits the proliferation of mouse L1210 leukemia cells and human CCRF-CEM lymphoblastic leukemia cells with ED50 values of 0.79 and 2.7 nM, respectively[1]. The ED50 values determined for the parent cell line CCRF-CEM, CCRFCEM R30/6 subline, CCRF-CEM R1, and CCRF-CEM R2 are 2.7, 5.8, 94 and 76 nM, respectively[1].
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.
Cell Viability Assay[1]
Cell Line:
L1210 and CCRF-CEM cells
Concentration:
0.1, 0.3, 1, 3, and 10 nM for L1210 cells; 0.3, 1, 3, 10, and 30 for CCRF-CEM cells
Incubation Time:
48 hours for L1210 cells; 72 hours for CCRF-CEM cells
Result:
The ED50 values were 0.79 and 2.7 nM for L1210 and CCRF-CEM cells, respectively.
分子量
440.45
Formula
C21H24N6O5
CAS 号
125991-51-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. F Itoh ,et al. Novel pyrrolo[2,3-d]pyrimidine Antifolate TNP-351: Cytotoxic Effect on Methotrexate-Resistant CCRF-CEM Cells and Inhibition of Transformylases of De Novo Purine Biosynthesis. Cancer Chemother Pharmacol. 1994;34(4):273-9.
TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo[1].
IC50 & Target
Antifolate, DHFR[1]
体外研究 (In Vitro)
TNP-351 inhibits the proliferation of mouse L1210 leukemia cells and human CCRF-CEM lymphoblastic leukemia cells with ED50 values of 0.79 and 2.7 nM, respectively[1]. The ED50 values determined for the parent cell line CCRF-CEM, CCRFCEM R30/6 subline, CCRF-CEM R1, and CCRF-CEM R2 are 2.7, 5.8, 94 and 76 nM, respectively[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
L1210 and CCRF-CEM cells
Concentration:
0.1, 0.3, 1, 3, and 10 nM for L1210 cells; 0.3, 1, 3, 10, and 30 for CCRF-CEM cells
Incubation Time:
48 hours for L1210 cells; 72 hours for CCRF-CEM cells
Result:
The ED50 values were 0.79 and 2.7 nM for L1210 and CCRF-CEM cells, respectively.
分子量
440.45
Formula
C21H24N6O5
CAS 号
125991-51-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. F Itoh ,et al. Novel pyrrolo[2,3-d]pyrimidine Antifolate TNP-351: Cytotoxic Effect on Methotrexate-Resistant CCRF-CEM Cells and Inhibition of Transformylases of De Novo Purine Biosynthesis. Cancer Chemother Pharmacol. 1994;34(4):273-9.
TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.
IC50 & Target
methionine aminopeptidase-2[1], angiogenesis[2]
体外研究 (In Vitro)
No significant difference of apoptotic cell numbers is observed between cells treated with TNP-470 and the controls. The IC50s of TNP-470 are 16.86±0.9 µg/mL, 3.16±0.6 µg/mL and 1.78±0.8 µg/mL for KKU-M213 cells at 24, 48 and 72 h, respectively. The results show that TNP-470 significantly reduces the number of migrated cells and invaded cells as compare with the vehicle treated group. TNP-470 decreases the migrated cells of KKU-M213 to 26% and of KKU-M214 to 11% (P<0.01). Similarly, TNP-470 also significantly affects cell invasion, the number of invaded cells is reduced to 25% in KKU-M213 (P<0.01) and to 15% in KKU-M214 (P<0.01). The relative expressions of MMP2, MMP9 and c-MYC in TNP-470 treated cells are significantly suppressed compare to the vehicle treated cells[1].
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.
体内研究 (In Vivo)
Treatment with TNP-470 attenuates (P<0.05) liver lipid accumulation compare to high fat fed (HFF) mice. By day 5, TNP-470 treated mice consume significantly less grams of high fat food than vehicle treated HFF mice. By day 15 of treatment, TNP-470 mice are consuming an equivalent number of calories to that of chow fed mice, despite the provision of high fat diet. Treatment with TNP-470 increases (P<0.05) expression of adipose tissue LPL mRNA, compare to chow-fed and high-fat fed controls. TNP-470 decreases energy intake and increases energy expenditure[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.
Clinical Trial
分子量
401.88
Formula
C19H28ClNO6
CAS 号
129298-91-5
中文名称
夫马菌素醇;夫马吉欣
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Kidoikhammouan S, et al. TNP-470, a methionine aminopeptidase-2 inhibitor, inhibits cell proliferation, migration and invasion of human cholangiocarcinoma cells in vitro. Asian Pac J Cancer Prev. 2012;13 Suppl:155-60.
[2]. White HM, et al. The angiogenic inhibitor TNP-470 decreases caloric intake and weight gain in high-fat fed mice. Obesity (Silver Spring). 2012 Oct;20(10):2003-9.
Cell Assay [1]
MTT assays are applied to test cell viability. In brief, 3×103 cells per well are seeded in a 96-well plate and incubated with various concentration of TNP-470 for 24, 48, and 72 h at 37°C, 5% CO2. For comparison, cells cultured in the absence of TNP-470 are used as a control. After an incubation period, 10 μL MTT (0.5 mg/mL final concentration) is added to each well. After 4 h of additional incubation, 100 μL of 0.01 N HCl in isopropanol is added to dissolve the crystals. Absorption at 570 nm is determined by ELISA plate reader[1].
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 Administration [2]
Individually housed, 4 wk old male C57BL/6 mice are used in this study. After a 1 wk acclimation period, mice are randomly allocated to receive either standard chow diet or high-fat diet for 6.5 wk. Throughout the high-fat feeding period the mice are treated with TNP-470 at a dose of 20 mg/kg body weight, injected subcutaneously every other day (TNP; n=7) or a vehicle injection of an equivalent volume (HFF controls; n=7). Vehicle injections contain 3% ethanol in phosphate-buffered saline. Chow-fed control mice (chow; n=8) are sham injected. Mice are fed ad libitum with food replaced every 2 or 3 days. Body weights are collected three times per week. After 6.5 wk of feeding, animals are fasted for 16-h and sacrificed. Final body, liver, and epididymal adipose tissue weights are measured. Liver and adipose tissue samples are frozen in liquid nitrogen and stored at -80°C for subsequent analysis[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.
参考文献
[1]. Kidoikhammouan S, et al. TNP-470, a methionine aminopeptidase-2 inhibitor, inhibits cell proliferation, migration and invasion of human cholangiocarcinoma cells in vitro. Asian Pac J Cancer Prev. 2012;13 Suppl:155-60.
[2]. White HM, et al. The angiogenic inhibitor TNP-470 decreases caloric intake and weight gain in high-fat fed mice. Obesity (Silver Spring). 2012 Oct;20(10):2003-9.
TNP is a cell-permeable inhibitor of IP6K1 and IP3K, with IC50 values of 0.55 µM and 10.2 µM for IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes[1].
IC50 & Target
IC50: 0.55 µM (IP6K1), 10.2 μM (IP3K)[1].
分子量
443.38
Formula
C20H16F3N7O2
CAS 号
519178-28-0
运输条件
Room temperature in continental US; may vary elsewhere.