FIT-039|cas:1113044-49-7|西域试剂

FIT-039,99.56%

产品编号：Bellancom-18944| CAS NO：1113044-49-7| 分子式：C₁₇H₁₈FN₃S| 分子量：315.41

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-18944	￥900.00	杭州北京（现货）
Bellancom-18944	￥1500.00	杭州北京（现货）
Bellancom-18944	￥3000.00	杭州北京（现货）
Bellancom-18944	￥4800.00	杭州北京（现货）
Bellancom-18944	￥7700.00	杭州北京（现货）

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FIT-039

产品介绍

FIT-039 是一种选择性，ATP 竞争性且具有口服活性的 CDK9 抑制剂，对 CKD9/cyclin T1 的 IC₅₀ 为 5.8 μM。FIT-039 不抑制其他 CDK 和其他激酶。FIT-039 抑制 HSV-1 (IC₅₀ 为 0.69 μM)，HSV-2，人腺病毒和人 CMV 的复制。FIT-039 是一种有前途的抗病毒剂，可用于抑制耐药性 HSV 和其他 DNA 病毒。

生物活性

FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC₅₀ of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC₅₀ of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.

体外研究

FIT-039 (30 μM; 3 hours; HEK293 cells) treatment decreases phosphorylated CTD in the infected or noninfected cells to a level lower than that shown by Flavopiridol. FIT-039 reduces the expression levels of HSV-1 immediate-early genes (IEGs) and early and late genes.
FIT-039 inhibits replication of the HSV-1 genome in a dose-dependent manner (EC₅₀ and EC₈₀ are 0.69 μM and 4.0 μM, respectively).
FIT-039 potently suppresses 8 kinases (GSK3β, PKN1, haspin, p70s6K, DYRK1B, GSK3α, IRR, and DYRK3) other than CDK9 on the 332-kinase panel. These kinases are involved in the replication of various viruses.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	HEK293 cells
Concentration:	30 μM
Incubation Time:	3 hours
Result:	Decreased phosphorylated carboxyterminal domain (CTD) in the infected or noninfected cells to a level lower than that shown by Flavopiridol.

体内研究
(In Vivo)

Treatment with the FIT-039 ointment twice a day suppresses skin lesions and rescues mice (male BALB/c mice injected with HSV-1) from lethality in a dose-dependent manner. The healing of lesions is observed with 5% to 10% FIT-039 ointment, leading to the complete regression of zosteriform spread on day 10, which is also observed with the 5% ACV ointment.
FIT-039 does not affect body weight gain in mice administrated with an overdose of this compound (1000 mg/kg/d) for 14 days, and no changes are observed in biological markers in their blood.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (317.05 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1705 mL	15.8524 mL	31.7048 mL
5 mM	0.6341 mL	3.1705 mL	6.3410 mL
10 mM	0.3170 mL	1.5852 mL	3.1705 mL

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (7.93 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.93 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (7.93 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.93 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.93 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。