KSI-3716 500mg

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Qiagen 凯杰 Biosharp Omega

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首页酶、辅酶及抑制剂MCE>

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商品介绍
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KSI-3716是 c-Myc 的抑制剂。

Description

KSI-3716 is a c-Myc inhibitor.

IC₅₀ & Target

c-Myc^[1]

In Vitro

KSI-3716 blocks c-MYC/MAX from forming a complex with target gene promoters. KSI-3716 effectively blocks complex formation in a dose dependent manner (IC₅₀=0.84 μM). c-MYC mediated transcriptional activity is inhibited by KSI-3716 at concentrations as low as 1 μM. The expression of c-MYC target genes, such as cyclin D2, CDK4 and hTERT, is markedly decreased. KSI-3716 exerts cytotoxic effects on bladder cancer cells by inducing cell cycle arrest and apoptosis^[1].

In Vivo

Intravesical instillation of KSI-3716 at a dose of 5 mg/kg significantly suppresses tumor growth with minimal systemic toxicity^[1].

Solvent & Solubility

In Vitro:

10 mM in DMSO

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3469 mL	11.7346 mL	23.4692 mL
5 mM	0.4694 mL	2.3469 mL	4.6938 mL
10 mM	0.2347 mL	1.1735 mL	2.3469 mL

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

References

[1]. Jeong KC, et al. Intravesical instillation of c-MYC inhibitor KSI-3716 suppresses orthotopic bladder tumor growth. J Urol. 2014 Feb;191(2):510-8.

Cell Assay ^[1]	Ku19-19 cells are seeded 1 day before drug treatment and treated with KSI-3716 (5, 10, 15, 20, 25 μM) for (12, 24, 48 hours). Cell survival assays are performed to count viable cells^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] ^[1]The control group is administered solvent and the experimental group (5 tumor bearing mice per group) is administered c-MYC inhibitor KSI-3716 (5 mg/kg) intravesically twice weekly for 3 weeks. Luminescence images are obtained twice weekly^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Jeong KC, et al. Intravesical instillation of c-MYC inhibitor KSI-3716 suppresses orthotopic bladder tumor growth. J Urol. 2014 Feb;191(2):510-8.

Molecular Weight	426.09
Formula	C₁₇H₁₁BrCl₂N₂O₂
CAS No.	1151813-61-4
SMILES	ClC1=CC=C(Br)C(NC(NC2=CC=C(Cl)C=C2)=C3C(C)=O)=C1C3=O
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping	Room temperature in continental US; may vary elsewhere