I-BET567|cas:1887237-54-8|西域试剂

I-BET567,99.68%

产品编号：Bellancom-142520| CAS NO：1887237-54-8| 分子式：C₁₇H₁₈ClN₅O₂| 分子量：359.81

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-142520		￥7400.00	杭州北京（现货）
Bellancom-142520		￥11700.00	杭州北京（现货）

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I-BET567

产品介绍

I-BET567 是一种有效、具有口服活性 pan-BET 候选抑制剂，对 BRD4 BD1 和 BD2 的 pIC₅₀s 分别为 6.9 和 7.2。I-BET567 已在肿瘤和炎症小鼠模型中已被证明有效。

生物活性

I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC₅₀s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.

体外研究

I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) effectively inhibites the proliferation of human NMC cell line 11060 in vitro with a mean gpIC₅₀ 6.2 (0.63 μM).

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

Cell Viability Assay

Cell Line:	NMC line 11060 cells
Concentration:	1.5 nM-30 μM
Incubation Time:	72 hours
Result:	Significantly reduced cell growth.

体内研究
(In Vivo)

I-BET567 (compound 27) (3, 10, and 30 mg/kg; p.o.; once daily for 20 days) leads to a significant reduction in tumor growth compared with vehicle controls at both 10 and 30 mg/kg.
Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle dog^a.

species	dose iv^b/po^c (mg/kg)	CL^b (mL/min/kg)	CL^b,u (mL/min/kg)	CL^renal (mL/min/kg)	V_ss (L/kg)	V_ss,u (L/kg)	t_1/2 (h)	Fpo (%)	f_ub
rat	1.3/3	25	109	7	2.4	10.4	1.6	99^d	0.23
dog	1.0/3	8.1	20	6.9	1.2	2.9	1.8	98	0.41

a: Values are mean, n=3 unless otherwise stated. b: IV dose 1h infusion in DMSO and (10%, w/v) Kleptose HPB in saline (2%: 98% (v/v)). c: PO dose vehicle: 1%(w/v) methycellulose (400 cps) (aq). d: Mean n = 2.

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

Animal Model:	NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells)
Dosage:	3, 10, and 30 mg/kg
Administration:	p.o. (once daily for 20 days
Result:	Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg.

体内研究

species	dose iv^b/po^c (mg/kg)	CL^b (mL/min/kg)	CL^b,u (mL/min/kg)	CL^renal (mL/min/kg)	V_ss (L/kg)	V_ss,u (L/kg)	t_1/2 (h)	Fpo (%)	f_ub
rat	1.3/3	25	109	7	2.4	10.4	1.6	99^d	0.23
dog	1.0/3	8.1	20	6.9	1.2	2.9	1.8	98	0.41

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

Animal Model:	NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells)
Dosage:	3, 10, and 30 mg/kg
Administration:	p.o. (once daily for 20 days
Result:	Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg.

体内研究

species	dose iv^b/po^c (mg/kg)	CL^b (mL/min/kg)	CL^b,u (mL/min/kg)	CL^renal (mL/min/kg)	V_ss (L/kg)	V_ss,u (L/kg)	t_1/2 (h)	Fpo (%)	f_ub
rat	1.3/3	25	109	7	2.4	10.4	1.6	99^d	0.23
dog	1.0/3	8.1	20	6.9	1.2	2.9	1.8	98	0.41

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

Animal Model:	NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells)
Dosage:	3, 10, and 30 mg/kg
Administration:	p.o. (once daily for 20 days
Result:	Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (277.92 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7792 mL	13.8962 mL	27.7924 mL
5 mM	0.5558 mL	2.7792 mL	5.5585 mL
10 mM	0.2779 mL	1.3896 mL	2.7792 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 (protect from light)。-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 (6.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.95 mM，饱和度未知) 的澄清溶液。
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 (6.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.95 mM，饱和度未知) 的澄清溶液。
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 (6.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.95 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。