RGB-286638 - CAS:784210-87-3

您当前的位置：

RGB-286638

目录号 : KM11289 CAS No. : 784210-87-3 纯度 : 98%

Data Sheet 产品使用指南

RGB-286638 是一种有效的 CDK 抑制剂，抑制 cyclin T1-CDK9，cyclin B1-CDK1，cyclin E-CDK2，cyclin D1-CDK4，cyclin E-CDK3 和 p35-CDK5 活性，IC₅₀ 分别为 1，2，3，4，5 和 5 nM；同时可抑制 GSK-3β，TAK1，Jak2 和 MEK1，IC₅₀ 值分别为 3，5，50，和 54 nM。

规格	价格	是否有货
2mg		In-stock
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

查看所有商品（2）

加入购物车大包装询价

Other Forms of Rapamycin:

Ginkgolide B In-stock
Isoginkgetin In-stock
Ginkgolic acid C17:1 In-stock
Ginkgolic Acid In-stock
Propargyl-PEG4-amine In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC₅₀s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC₅₀s of 3, 5, 50, and 54 nM.

体外研究

RGB-286638 is an indenopyrazole-derived CDK inhibitor (CDKI) with K_i-nanomolar activity against transcriptional CDKs. RGB-286638 inhibits several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. The dose- and time-dependent effect of treatment with RGB-286638 (12.5-100nM) is investigated on the growth of human p53-wt (MM.1S, MM.1R, and H929) and p53-mutant (U266, OPM1, and RPMI) MM cells by MTT assay, assessing viability at 24 and 48 hours. The half-maximally effective concentrations (EC₅₀) range between 20 and 70 nM at 48 hours. Dose-dependent differences in growth among p53-wt and -mutant cells are observed after 50nM treatment, with p53-wt MM.1S, MM.1R and H929 being slightly more sensitive to RGB-286638 treatment at 48h.

体内研究

Dose-finding studies with RGB-286638 identify 40 mg/kg/day IV treatment as the maximum tolerated dose in SCID mice. Five days IV treatment with RGB-286638 significantly suppresses MM tumor growth, with maximum TGI (%) noted at day 14 following end of treatment at 85.06% and 86.34% in the 30 mg/kg and 40 mg/kg treated cohorts respectively. The log10 cell kill (LCK Td: 4.5 days) is 1.6 for both treated groups. RGB-286638 treatment is also associated with improved survival, evidenced by first death at day 24 in controls versus day 43 in both treated groups. No toxic deaths occurred during this study: maximum percentage of body weight (BW) loss is observed on day 5 (8.4%) at 30 mg/kg dosage schedule, and on day 15 (9.9%) after 40 mg/kg dosing, with weight recovery in the following two weeks.

分子式

C₂₉H₃₇Cl₂N₇O₄

分子量

618.55

CAS号

784210-87-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 150 mg/mL (242.50 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6167 mL	8.0834 mL	16.1668 mL
5 mM	0.3233 mL	1.6167 mL	3.2334 mL
10 mM	0.1617 mL	0.8083 mL	1.6167 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: ≥ 7.5 mg/mL (12.13 mM); Clear solution

此方案可获得 ≥ 7.5 mg/mL (12.13 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 75.0 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 7.5 mg/mL (12.13 mM); Clear solution

此方案可获得 ≥ 7.5 mg/mL (12.13 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 75.0 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。