BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC₅₀ of 0.19 nM and a K_i of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC₅₀ of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research^[1].

BMS-986202 inhibits IFNα and IL-23 in Kit225 T cells with IC₅₀ values of 10 nM and 12 nM, respectively^[1].
BMS-986202 is potent in the IFNα stimulated STAT5 phosphorylation human whole blood (hWB) assay and mouse whole blood (mWB) with IC₅₀ values of 58 nM and 481 nM, respectively^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-986202 (Compound 7; 3-30 mg/kg; p.o.; daily; for 9 days) treatment inhibits IL-23-driven acanthosis in mice^[1].
BMS-986202 (Compound 7; 0.4-10 mg/kg; p.o.) treatment inhibits IL-12/IL-18-induced IFNγ production in mice. BMS-986202 dose-dependently inhibits IFNγ production by 46% and 80% at doses of 2 mg/kg and 10 mg/kg, respectively^[1].
BMS-986202 (Compound 7; 7-10 mg/kg; p.o.) is stable in liver microsomes, with half lives of greater than 120 min in mouse, rat, monkey, and humans and 89 min in dog. The serum protein binding for BMS-986202 in these species ranges from 89.3% to 96.0%, leaving a good range of free fraction of drug available. BMS-986202 shows the oral bioavailability up to 62-100%^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

439.46

C₂₂H₁₈D₃FN₆O₃

1771691-34-9

Room temperature in continental US; may vary elsewhere.

DMSO : 250 mg/mL (568.88 mM; Need ultrasonic)

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。

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: ≥ 2.08 mg/mL (4.73 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.73 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

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.73 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。

• [1]. Chunjian Liu, et al. Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2. J Med Chem. 2021 Jan 14;64(1):677-694.