Birinapant 纯度:99.84% 2mg

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Birinapant 纯度:99.84% 2mg

市场价：: 850.00

促销价：: ¥850.00

货号：HY-16591

品牌：MCE

配送至：

北京朝阳

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商品介绍
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Birinapant是一种二价Smac模拟物，是 XIAP 和 cIAP1 的强效拮抗剂，K_d 值分别为45 nM和小于1 nM。

Description

Birinapant, a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with K_ds of 45 nM and less than 1 nM, respectively.

IC₅₀ & Target

Kd: 45 nM (XIAP), <1 nM (cIAP1)

In Vitro

Birinapant causes significant degradation of cIAP1 and 2. Birinapant + TRAIL-treated cells show increased levels of active caspase-8 and caspase-3, as well as PARP cleavage, over single agents within 4 h of treatment, indicative of apoptosis-mediated cell death. Birinapan significantly decreases the viability of SUM190 cells in a dose-dependent manner. Birinapant treatment in the XIAP knockdown cell line (SUM190 shXIAP) causes an overall reduction in viability at lower doses (30-300 nM)^[1]. Birinapant causes apoptosis in the sensitive cells. Birinapant in conbination with TNF-α, causes PARP cleavage in 451Lu and WM1366 cell lines^[2]. Birinapant induces time-course of caspase-3 activation in HCT116 human colon carcinoma and MDA-MB-231 human breast adenocarcinoma cells^[3].

In Vivo

Birinapant can inhibit tumor growth in melanoma xenotransplantation models. Staining for activated caspase-3 in biopsies of the same tumors show a modest increase in apoptotic cells in the birinapant treated animals^[2]. Birinapant (15 mg/kg, i.p.) induces apoptosis in HCT116 tumor-bearing mouse^[3].

Solvent & Solubility

In Vitro:

DMSO : ≥ 40 mg/mL (49.57 mM)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.2392 mL	6.1962 mL	12.3925 mL
5 mM	0.2478 mL	1.2392 mL	2.4785 mL
10 mM	0.1239 mL	0.6196 mL	1.2392 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (2.58 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (2.58 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (2.58 mM); Suspended solution; Need ultrasonic

References

[1]. Allensworth JL, et al. Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism. Breast Cancer Res Treat. 2013 Jan;137(2):359-71.

[2]. Krepler C, et al. The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells. Clin Cancer Res. 2013 Apr 1;19(7):1784-94.

[3]. Nguyen QD, et al. Temporal and spatial evolution of therapy-induced tumor apoptosis detected by caspase-3-selective molecular imaging. Clin Cancer Res. 2013 Jul 15;19(14):3914-24.

Cell Assay ^[1]	Trypan blue exclusion assay is performed as described. Cells are seeded in 6 well plates at 7.5×10⁴ (SUM149) or 1.5×10⁵ (SUM190) cells per well and allowed to adhere overnight. Cells are treated with TRAIL (0-100 ng/mL), Birinapant (0-10,000 nM), GT13402 (0-10,000 nM), TNF-α (50 ng/mL), TNF-α neutralizing antibody (10 μg/mL), pan-caspase inhibitor Q-VD-OPh (20 μM), or a combination as indicated. All treatments are applied for 24 h, and then the cells are trypsinized and resuspended in PBS. Next, 10 μL of cell suspension is added to 10 μL 0.4 % trypan blue, and 10 μL of the mixture is loaded onto a hemocytometer; cells are counted, and live and dead cell numbers are recorded. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Ten animals each are inoculated s.c. with 1×10⁶ 451Lu or 1205Lu human melanoma cells in a suspension of matrigel/complete media at a ratio of 1:1. After formation of palpable tumors, mice from both tumor models are randomized into two groups. Both groups are treated intraperitoneal three times/week with either vehicle control or birinapant 30 mg/kg for 21 days. Birinapant is dissolved in 12.5% Captisol in distilled water. Tumor size is assessed twice weekly by caliper measurement. Subsequently, satellite groups of ten and fifteen mice are inoculated in the same fashion with 451Lu and 1205Lu tumor cells respectively. After tumors have reached a mean volume of 200 mm³ animals are dosed with either birinapant or vehicle control as described above. After 48 hours and two doses, animals are sacrificed and tumors are harvested at four time points after the last treatment. Tumor samples are snap frozen in liquid nitrogen for subsequent protein analysis and preserved as FFPE blocks for immune-histochemistry. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Allensworth JL, et al. Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism. Breast Cancer Res Treat. 2013 Jan;137(2):359-71. [2]. Krepler C, et al. The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells. Clin Cancer Res. 2013 Apr 1;19(7):1784-94. [3]. Nguyen QD, et al. Temporal and spatial evolution of therapy-induced tumor apoptosis detected by caspase-3-selective molecular imaging. Clin Cancer Res. 2013 Jul 15;19(14):3914-24.

Molecular Weight

806.94

Formula

C₄₂H₅₆F₂N₈O₆

CAS No.

1260251-31-7

SMILES

FC1=CC2=C(C=C1)C(C[C@H]3N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C3)=C(C(N4)=C(C[C@H]5N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C5)C6=C4C=C(F)C=C6)N2

Storage