C078157
3-aminopyridine-2-carboxaldehyde thiosemicarbazone
CAS: 143621-35-6
Molecular Formula: C7H9N5S
C078157 - Names and Identifiers
C078157 - Physico-chemical Properties
| Molecular Formula | C7H9N5S |
| Molar Mass | 195.24 |
| Density | 1.46±0.1 g/cm3(Predicted) |
| Melting Point | 234 °C |
| Boling Point | 436.0±55.0 °C(Predicted) |
| Solubility | DMSO: soluble10Meq/mL, clear |
| Appearance | powder |
| Color | white to light brown |
| pKa | 10.93±0.70(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | 3-AP (Triapine) is a potent derivative of α-heterocyclic carboxaldehyde thiosemicarbazone (HCT) that inhibits hRRM2 and p53R2 isoforms of the M2 subunit. 3-AP (Triapine) is thought to inhibit ribonucleotide reductase through its preformed iron chelate, rather than directly by removing iron from the active site. In cells containing less topoisomerase IIα fewer DNA strand breaks will be produced, and thus topoisomerase II poisons will be less inhibitory in the K/VP.5 cell line. The IC 50 s for Dp44mT growth inhibition are 48±9 nM and 60±12 nM, for K562 and K/VP.5 cells, respectively. The IC 50 s for 3-AP growth inhibition are 476±39 nM and 661±69 nM for K562 and K/VP.5 cells, respectively. PKIH and DpT Fe chelators show high antiproliferative activity against a range of tumor cell lines. Dp44mT shows the greatest antitumor efficacy with an IC 50 that ranged from 0.005 to 0.4 μM. The average IC 50 of Dp44mT over 28 cell types is 0.03±0.01 μM, which is significantly lower than that of 3-AP (Triapine; average IC 50 : 1.41±0.37 μM). |
| In vivo study | 3-AP (Triapine) causes a significant increase (1.7-fold) in splenic weight when expressed as a percentage of total body weight (1.02±0.06%; n=25) compared with control mice (0.6±0.03%; n=27). In the long-term group, a significant increase in heart weight is observed after Dp44mT (0.4 mg/kg per day) (0.8±0.06%; n=4) compared with control mice (0.5±0.01%; n=6). A significant decrease in the expression of Ndrg1, TfR1, and VEGF1 in the liver is noted for Dp44mT- and 3-AP (12 mg/kg per day)-treated animals. The decreased expression could be related to the increased liver Fe in both Dp44mT- and 3-AP-treated mice. |
C078157 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
| Toxicity | LDLo ivn-rat: 20 mg/kg IJTOFN 19,85,2000 |
C078157 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 5.122 ml | 25.609 ml | 51.218 ml |
| 5 mM | 1.024 ml | 5.122 ml | 10.244 ml |
| 10 mM | 0.512 ml | 2.561 ml | 5.122 ml |
| 5 mM | 0.102 ml | 0.512 ml | 1.024 ml |
Last Update：2024-01-02 23:10:35
C078157 - Reference Information
| biological activity | 3-AP (PAN-811) is a ribonucleotide reductase (RR) the M2 subunit inhibitor is a potent radiosensitizer. |
| Target | ribosucletide reductase (RR) |
Last Update：2024-04-09 19:05:17
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Product Name: 3-AP Visit Supplier Webpage Request for quotationCAS: 143621-35-6
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: 3-aminopyridine-2-carboxaldehyde thiosemicarbazone Visit Supplier Webpage Request for quotationCAS: 143621-35-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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