Dalpiciclib hydrochloride SHR-6390 hydrochloride|西域试剂

Dalpiciclib hydrochloride SHR-6390 hydrochloride,99.92%

产品编号：Bellancom-114338A| 分子式：C₂₅H₃₁ClN₆O₂| 分子量：483.01

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货号	价格	库存与货期
Bellancom-114338A	￥4600.00	杭州北京（现货）
Bellancom-114338A	￥7300.00	杭州北京（现货）
Bellancom-114338A	￥14600.00	杭州北京（现货）

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Dalpiciclib hydrochloride SHR-6390 hydrochloride

产品介绍

Dalpiciclib (SHR-6390) hydrochloride 是一种具有口服活性和高选择性的 CDK4/6 抑制剂，IC₅₀ 值分别为 12.4 nM 和 9.9 nM。Dalpiciclib hydrochloride 对乳腺癌和食道鳞状细胞癌显示出抗肿瘤活性。

生物活性

Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC₅₀ values of 12.4 nM and 9.9 nM, respectively. Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma^[4].

体外研究

Dalpiciclib hydrochloride (0-4 μM, 72 h) inhibits cell proliferation in a dose-dependent manner.
Dalpiciclib hydrochloride (0-10 μM, 6 d) inhibits the proliferation of retinoblastoma-positive tumor cell lines^[4].

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

Cell Proliferation Assay

Cell Line:	Eca 109, Eca 9706 and KYSE-510 ESCC cell lines
Concentration:	0-4 μM
Incubation Time:	72 hours
Result:	Inhibited cell proliferation in a dose-dependent manner, with Eca 109 being the relative sensitive one and Eca 9706 being the relative resistant one.

Cell Viability Assay^[4]

Cell Line:	MCF7, MCF7/TR, BT-474/T cell lines
Concentration:	0-10 μM
Incubation Time:	6 days
Result:	Inhibited MCF7/TR cells, parental MCF7 cells and BT-474/T resistant cells with the IC₅₀ values of 229.5, 115.4 and 210.7 nM, respectively.

体内研究
(In Vivo)

Dalpiciclib hydrochloride (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts.
Dalpiciclib hydrochloride combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts.
Dalpiciclib hydrochloride (oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days) shows antitumor activity in human xenograft models ^[4].

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

Animal Model:	NOD/SCID mice (ESCC PDXs models)
Dosage:	150 mg/kg
Administration:	Oral gavage; 150 mg/kg; once weekly; 3 weeks
Result:	Suppressed the growth of tumor.

Animal Model:	5-week-old female Balb/cA-nude mice subcutaneously inoculated MCF7/ARO, COLO 205 and U87MG^[4]
Dosage:	37.5 mg/kg, 75 mg/kg, 150 mg/kg
Administration:	Oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days
Result:	Caused regression of all tumor xenografts at the highest dose tested.

体内研究

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

Animal Model:	NOD/SCID mice (ESCC PDXs models)
Dosage:	150 mg/kg
Administration:	Oral gavage; 150 mg/kg; once weekly; 3 weeks
Result:	Suppressed the growth of tumor.

Animal Model:	5-week-old female Balb/cA-nude mice subcutaneously inoculated MCF7/ARO, COLO 205 and U87MG^[4]
Dosage:	37.5 mg/kg, 75 mg/kg, 150 mg/kg
Administration:	Oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days
Result:	Caused regression of all tumor xenografts at the highest dose tested.

体内研究

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

Animal Model:	NOD/SCID mice (ESCC PDXs models)
Dosage:	150 mg/kg
Administration:	Oral gavage; 150 mg/kg; once weekly; 3 weeks
Result:	Suppressed the growth of tumor.

Animal Model:	5-week-old female Balb/cA-nude mice subcutaneously inoculated MCF7/ARO, COLO 205 and U87MG^[4]
Dosage:	37.5 mg/kg, 75 mg/kg, 150 mg/kg
Administration:	Oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days
Result:	Caused regression of all tumor xenografts at the highest dose tested.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (10.35 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0704 mL	10.3518 mL	20.7035 mL
5 mM	0.4141 mL	2.0704 mL	4.1407 mL
10 mM	0.2070 mL	1.0352 mL	2.0704 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献