TL 32711
Birinapant
CAS: 1260251-31-7
Molecular Formula: C42H56F2N8O6
TL 32711 - Names and Identifiers
TL 32711 - Physico-chemical Properties
| Molecular Formula | C42H56F2N8O6 |
| Molar Mass | 806.94 |
| Density | 1.320±0.06(20.0000℃) |
| Melting Point | >245oC (dec.) |
| Boling Point | 1090.5±65.0 °C(Predicted) |
| Solubility | Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 13.99±0.46(Predicted) |
| Storage Condition | -20°C Freezer |
| Use | Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist of XIAP and cIAP1 with Kd values of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces self-ubiquitination and proteasome degradation of cIAP1 and cIAP2 in intact cells, resulting in the formation of RIPK1: caspase-8 complexes, caspase-8 activation and induction of tumor cell death. Birinapant (TL32711) targeted TRAF2-related cIAP and abolished TNF-induced NF-κB activation. |
| In vitro study | The Kd of Birinapant binding to XIAP and CIAP1 was 45 nM and <1 nM, respectively. In TRAIL-insensitive SUM190 (overexpression of ErbB2) cells, Birinapant alone induces cell death (IC 50 is approximately 300 nM), and significantly increased TRAIL-induced apoptosis of TRAIL-sensitive SUM149 (triple negative, EGFR activated) cells. Birinapant results in rapid degradation of CIAP1, caspase activation, PARP cleavage, and activation of NF-κB. Birinapant in combination with TNF-α showed a strong anti-melanoma effect in vitro. The combination of Birinapant and TNF-α(1 ng/mL) inhibited the growth of the human melanoma cell lines WTH202,WM793B, wmartemisinin and WM164 with IC50 of 1.8,2.5,7.9 and 9 nM, respectively, both compounds alone were ineffective. Birinapant treatment alone induced inhibition of WM9 cell proliferation with IC 50 at 2.4 nM. Birinapant significantly inhibited the target proteins CIAP1 and cIAP2 in these cell lines. The K d of Birinapant binding to XIAP and CIAP1 was 45 nM and <1 nM, respectively. In TRAIL-insensitive SUM190 (overexpression of ErbB2) cells, Birinapant alone induces cell death (IC 50 is approximately 300 nM), and significantly increased TRAIL-induced apoptosis of TRAIL-sensitive SUM149 (triple negative, EGFR activated) cells. Birinapant results in rapid degradation of CIAP1, caspase activation, PARP cleavage, and activation of NF-κB. Birinapant in combination with TNF-α showed a strong anti-melanoma effect in vitro. The combination of Birinapant and TNF-α(1 ng/mL) inhibited the growth of the human melanoma cell lines WTH202,WM793B, wmartemisinin and WM164 with IC50 of 1.8,2.5,7.9 and 9 nM, respectively, both compounds alone were ineffective. Birinapant treatment alone induced inhibition of WM9 cell proliferation with IC 50 at 2.4 nM. Birinapant significantly inhibited the target proteins CIAP1 and cIAP2 in these cell lines. |
| In vivo study | Birinapant(30 mg/kg) significantly induced tumor growth in the malignant melanoma xenograft model 451LU. Birinapant(30 mg/kg) significantly induced tumor growth in a malignant melanoma xenograft model 451LU. |
TL 32711 - Risk and Safety
| HS Code | 29339900 |
TL 32711 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.239 ml | 6.196 ml | 12.392 ml |
| 5 mM | 0.248 ml | 1.239 ml | 2.478 ml |
| 10 mM | 0.124 ml | 0.62 ml | 1.239 ml |
| 5 mM | 0.025 ml | 0.124 ml | 0.248 ml |
Last Update：2024-01-02 23:10:35
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