TH-302
TH-302
CAS: 918633-87-1
Molecular Formula: C9H16Br2N5O4P
TH-302 - Names and Identifiers
TH-302 - Physico-chemical Properties
| Molecular Formula | C9H16Br2N5O4P |
| Molar Mass | 449.04 |
| Density | 1.97 |
| Melting Point | 97-98°C |
| Boling Point | 565.4±60.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | Off-White to Pale Yellow |
| pKa | 0.34±0.70(Predicted) |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| In vitro study | TH-302 is a hypoxia-activated prodrug that is currently in clinical evaluation. In the case of oxygen, the effect of TH-302 on the oval cells is much stronger than that of the single molecular layer. Under aerobic conditions, TH-302 is very effective and stable in liver microsomes. In the environment of N 2, TH-302 acts on human lung cancer H460 cells and human colon cancer HT29 cells, with high toxicity. TH-302, the IC90 of H460 cells and HT29 cells was 0.1 and 0.2 μm, respectively. TH-302 action on multiple myeloma is hypoxia-selective and dose-dependent. Under hypoxic conditions, TH-302 induced cell cycle to stop at G0/G1 phase. Regulation of p21cip-1 effects on the cell cycle by down-regulating cyclin D1/2/3, CDK4/6, p27kip-1, TH-302, and pRb expression, for which CDK2 expression has no effect. Under hypoxic conditions, TH-302 acts on human and murine multiple myeloma cells to induce apoptosis in a dose-dependent manner. BCL-2 activated apoptosis is regulated by down-regulating the expression of anti-apoptotic proteins BCL-xL and TH-302, as well as up-regulating the cleaved apoptosis precursor proteins caspase-3,-8, and -9, and PARP. Compared with the special toxicity in low oxygen environment, TH-302 showed low toxicity in normal oxygen environment or high oxygen environment. |
| In vivo study | On the 25th day of experimental transplantation, TH302 inhibited tumor growth by 41%, but the combination of TH302 and gemcitrate inhibited tumor growth by 96%. TH-302, H460 NSCLC transplantation model was injected intraperitoneally at a dose of 6.25, 12.5, 25, or 50 mg/kg, and treated once a day, 5 times a week for 2 weeks, tumor growth inhibition rates were 43%, 51%, 75%, and 89%, respectively. At a dose of 100 mg/kg on blood cells on TH-302, blood cells decreased 3 days after treatment, but completely recovered 7 days after treatment. TH-302 induced cell death, depending on the oxygen concentration, as for tumor-bearing mice in low oxygen concentration environment, the highest toxicity. The effect on animals requiring 10% O 2 for breathing oxygen TH-302 inhibited tumor growth significantly less than that in animals requiring 95% O 2 for breathing. At 48 hours after treatment on TH-302, pimonidazole-positive areas were significantly reduced (6.3±1.2% in the control group and 1.8±1.1% in the experimental group on TH-302). |
TH-302 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.227 ml | 11.135 ml | 22.27 ml |
| 5 mM | 0.445 ml | 2.227 ml | 4.454 ml |
| 10 mM | 0.223 ml | 1.113 ml | 2.227 ml |
| 5 mM | 0.045 ml | 0.223 ml | 0.445 ml |
Last Update：2024-01-02 23:10:35
TH-302 - Reference Information
| biological activity | Evofosfamide (TH-302) is a selective hypoxia-activated prodrug, targeting the hypoxic region of solid tumors, the IC50 is 19 nM, the cytotoxicity is enhanced 270 times under hypoxic conditions than under aerobic conditions, and the cytochrome P450 metabolism is stable. |
| in vitro study | TH-302 is a hypoxia-activated prodrug currently in clinical evaluation. In the case of oxygen, the effect of TH-302 on the oval cells is much stronger than that of the single molecular layer. Under aerobic conditions, TH-302 is very effective and stable in liver microsomes. In the environment of N 2, TH-302 acts on human lung cancer H460 cells and human colon cancer HT29 cells, with high toxicity. TH-302, the IC90 of H460 cells and HT29 cells was 0.1 and 0.2 μm, respectively. TH-302 action on multiple myeloma is hypoxia-selective and dose-dependent. Under hypoxic conditions, TH-302 induced cell cycle to stop at G0/G1 phase. Regulation of p21cip-1 effects on the cell cycle by down-regulating cyclin D1/2/3, CDK4/6, p27kip-1, TH-302, and pRb expression, for which CDK2 expression has no effect. Under hypoxic conditions, TH-302 acts on human and murine multiple myeloma cells to induce apoptosis in a dose-dependent manner. BCL-2 activated apoptosis is regulated by down-regulating the expression of anti-apoptotic proteins BCL-xL and TH-302, as well as up-regulating the cleaved apoptosis precursor proteins caspase-3,-8, and -9, and PARP. Compared with the special toxicity in low oxygen environment, TH-302 showed low toxicity in normal oxygen environment or high oxygen environment. |
| in vivo study | on the 25th day of experimental transplantation, TH302 inhibited tumor growth with an inhibition rate of 41%, however, the combination of TH302 and gemcitrate inhibited tumor growth by 96%. TH-302, H460 NSCLC transplantation model was injected intraperitoneally at a dose of 6.25, 12.5, 25, or 50 mg/kg, and treated once a day, 5 times a week for 2 weeks, tumor growth inhibition rates were 43%, 51%, 75%, and 89%, respectively. At a dose of 100 mg/kg on blood cells on TH-302, blood cells decreased 3 days after treatment, but completely recovered 7 days after treatment. TH-302 induced cell death, depending on the oxygen concentration, as for tumor-bearing mice in low oxygen concentration environment, the highest toxicity. The effect on animals requiring 10% O 2 for breathing oxygen TH-302 inhibited tumor growth significantly less than that in animals requiring 95% O 2 for breathing. At 48 hours after treatment on TH-302, pimonidazole-positive areas were significantly reduced (6.3±1.2% in the control group and 1.8±1.1% in the experimental group on TH-302). |
Last Update：2024-04-09 20:49:11
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