KB-0742 dihydrochloride|cas:2416874-75-2|西域试剂

KB-0742 dihydrochloride,99.63%

产品编号：Bellancom-137478A| CAS NO：2416874-75-2| 分子式：C₁₆H₂₇Cl₂N₅| 分子量：360.33

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-137478A	￥2600.00	杭州北京（现货）
Bellancom-137478A	￥4500.00	杭州北京（现货）
Bellancom-137478A	￥8000.00	杭州北京（现货）
Bellancom-137478A	￥14000.00	杭州北京（现货）

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KB-0742 dihydrochloride

产品介绍

KB-0742 dihydrochloride 是一种有效的，选择性的和具有口服活性的 CDK9 抑制剂，对 CDK9/cyclin T1 的 IC₅₀ 为 6 nM。KB-0742 dihydrochloride 对 CDK9/cyclin T1 具有选择性，其选择性是其他 CDK 激酶的 50 倍以上。KB-0742 dihydrochloride 具有有效的抗肿瘤活性。

生物活性

KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC₅₀ of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.

体外研究

KB-0742 (6 hours; 0.1-10 μM; 22Rv1 cells) treatment significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5. Global androgen receptor (AR)-FL and AR-V protein levels are significantly reduced starting at 6 h treatment time, which is accompanied by the reduction of phospho-AR levels (Ser81).
KB-0742 (48-72 hours) treatment shows cytostatic effects in prostate cancer and leukemia cell lines. KB-0742 shows antiproliferative activity with GR₅₀s of 0.183 μM and 0.288 μM for 22Rv1 cells and MV-4-11 AML cells, respectively.
In 22Rv1 cells, KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs.

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

Western Blot Analysis

Cell Line:	22Rv1 cells
Concentration:	0.1 μM, 0.5 μM, 1 μM, 10 μM
Incubation Time:	6 hours
Result:	Significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5.

体内研究
(In Vivo)

KB-0742 (3-30 mg/kg; p.o.; daily; over 21 days) is well tolerated even at high dose, while significantly reducing tumor burden in 22Rv1 human prostate cancer cell line-derived xenograft (CDX) models.

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

Animal Model:	Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells
Dosage:	3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:	p.o.; daily; over 21 days
Result:	Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC).

体内研究

KB-0742 (3-30 mg/kg; p.o.; daily; over 21 days) is well tolerated even at high dose, while significantly reducing tumor burden in 22Rv1 human prostate cancer cell line-derived xenograft (CDX) models.

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

Animal Model:	Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells
Dosage:	3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:	p.o.; daily; over 21 days
Result:	Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC).

体内研究

KB-0742 (3-30 mg/kg; p.o.; daily; over 21 days) is well tolerated even at high dose, while significantly reducing tumor burden in 22Rv1 human prostate cancer cell line-derived xenograft (CDX) models.

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

Animal Model:	Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells
Dosage:	3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:	p.o.; daily; over 21 days
Result:	Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC).

性状

Solid

溶解性数据

In Vitro:

H₂O : 100 mg/mL (277.52 mM; Need ultrasonic)

DMSO : 62.5 mg/mL (173.45 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7752 mL	13.8762 mL	27.7523 mL
5 mM	0.5550 mL	2.7752 mL	5.5505 mL
10 mM	0.2775 mL	1.3876 mL	2.7752 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 (sealed storage, away from moisture)。-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： PBS
Solubility: 100 mg/mL (277.52 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.77 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.77 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.77 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。