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AP20187 Sale

(Synonyms: B/B Homodimerizer) 目录号 : GC14498

A CID for FKBP fusion proteins

AP20187 Chemical Structure

Cas No.:195514-80-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥5,611.00
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1mg
¥864.00
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5mg
¥2,160.00
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10mg
¥3,440.00
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25mg
¥6,720.00
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50mg
¥10,400.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment: [1]

Cell lines

CHO-AA8-Tet off cells

Preparation method

The solubility of this compound in DMSO is >74.1mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

Applications

The cDNAs for the MLL-AF9 fusion protein were transfected in triplicate into CHO cells along with a Myc E box HSV TK luciferase reporter and a CMV-driven Renilla luciferase control plasmid. Results are expressed as a ratio of normalized firefly luciferase activity to the activity of cells transfected with an MSCV neomycin control vector. In the presence of the dimerizer AP20187, cells transfected with MLL-FKBP showed strong dose-dependent transactivation of the Myc E box HSV TK reporter. The dimerization of the fusion protein activated transcription with nearly 250-fold.

Animal experiment: [2]

Animal models

CD1 mice

Dosage form

Intraperitoneal injection, 10 mg/kg

Applications

To evaluate LFv2IRE expression and tyrosine phosphorylation, CD1 mice were injected via the tail vein with GC of AAV2/8-TBG-LFv2IRE or AAV2/1-MCK-LFv2IRE vector 4 weeks before the AP20187 injection. AP20187-dependent LFv2IRE tyrosine phosphorylation was evident 2 hr after drug administration, peaked 6 hr later, and returned to baseline after 24 hr. Low LFv2IRE basal phosphorylation was detected in liver samples from mice receiving AAV2/8-TBG-LFv2IRE but not stimulated with AP20187, suggesting minimal leakiness of the system.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Martin M E, Milne T A, Bloyer S, et al. Dimerization of MLL fusion proteins immortalizes hematopoietic cells. Cancer cell, 2003, 4(3): 197-207.

[2] Cotugno G, Formisano P, Giacco F, et al. AP20187-mediated activation of a chimeric insulin receptor results in insulin-like actions in skeletal muscle and liver of diabetic mice. Human gene therapy, 2007, 18(2): 106-117.

产品描述

AP20187 is a small dimerizer drug [1].

To solve the graft-versus-host disease, the in vivo behavior of the transplanted cells should be controlled. AP20187 is used in the conditional system as a chemical inducer of dimerization (CID). Another component is a fusion protein. The CIDs have advantages in gene therapy, it offers the possibility of achieving selection without the toxic effects. In vivo studies show that AP20187 can produces a notable expansion of transduced red cells, platelets, and to a lesser extent, granulocytes [1].

AP20187 is also reported to be used in an AP20187–LFv2IRE system. In this system, AP20187 administration causes the activation of LFv2IRE and results in increased uptake of both hepatic glycogen content and muscular glucose [2].

References:
[1] Neff T, Blau CA. Pharmacologically regulated cell therapy. Blood. 2001 May 1;97(9):2535-40.
[2] Cotugno G, Formisano P, Giacco F, Colella P, Beguinot F, Auricchio A. AP20187-mediated activation of a chimeric insulin receptor results in insulin-like actions in skeletal muscle and liver of diabetic mice. Hum Gene Ther. 2007 Feb;18(2):106-17.

Chemical Properties

Cas No. 195514-80-8 SDF
别名 B/B Homodimerizer
Canonical SMILES O=C([C@@H]1CCCCN1C([C@@H](CC)C2=CC(OC)=C(OC)C(OC)=C2)=O)O[C@H](CCC3=CC(OC)=C(OC)C=C3)C4=CC=CC(OCC(NCC(CNC(COC5=CC=CC([C@@H](CCC6=CC(OC)=C(OC)C=C6)OC([C@H]7N(C([C@@H](CC)C8=CC(OC)=C(OC)C(OC)=C8)=O)CCCC7)=O)=C5)=O)CN(C)C)=O)=C4
分子式 C82H107N5O20 分子量 1482.75
溶解度 ≥ 74.1375mg/mL in DMSO, ≥ 50mg/ml in 75% ethanol aqueous solution 储存条件 Store at -20°C,protect from light
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 0.6744 mL 3.3721 mL 6.7442 mL
5 mM 0.1349 mL 0.6744 mL 1.3488 mL
10 mM 0.0674 mL 0.3372 mL 0.6744 mL
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