TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC₅₀ of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC₅₀s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth^[1].

IC50: 0.03 nM (Fgr), 0.1 nM (Lyn) and 160 nM (Hck)^[1]

TL02-59 (0.1-1000 nM; 6 hours) potently inhibits Fgr autophosphorylation in TF-1 cells, with paritial inhibition at 0.1-1 nM and complete inhibition above 10 nM. Hck, Lyn and Flt3 are inhibited in the 100 to 1000 nM range^[1].
TL02-59 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency^[1].
TL02-59 induces growth arrest in primary AML bone marrow samples^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

TL02-59 (oral administration; 1 and 10 mg/kg; for three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement^[1].
TL02-59 has a t_1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

609.64

C₃₂H₃₄F₃N₅O₄

1315330-17-6

Room temperature in continental US; may vary elsewhere.

DMSO : 125 mg/mL (205.04 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 (3.41 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.41 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% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.41 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
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.41 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]. Weir MC, et al. Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. ACS Chem Biol. 2018 Jun 15;13(6):1551-1559.

TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC₅₀ value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC₅₀ values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984)^[1].

TL13-112 binds to cereblon with an IC₅₀ value of 2.4 uM^[1].
TL13-112 (0.01 μM-1 μM; 16 hours) is selective for degradation of ALK with the DC₅₀s of 10 nM and 40 nM in H3122 cell and Karpas 299, respectively. ALK degradation acts at 4 hours of treatment in H3122 cells and at 8 hours of treatment in Karpas 299 cells. The maximum degradation achieves at 16 hours in both cell lines. ^[1].
TL13-112 (0.01 μM-1 μM; 16 hours) inhibits PTK2, ALK, FER, RPS6KA1 and Aurora A expression as a dose-dependent manner in H3122, Karpas 299, and Kelly cells^[1].

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

1002.57

C₄₉H₆₀ClN₉O₁₀S

2229037-19-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Powell CE, et al. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).J Med Chem. 2018 May 10;61(9):4249-4255.

TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC₅₀ value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC₅₀ values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984)^[1].

TL13-12 (0-200 nM; 16 hours)  is selective for degradation of ALK with the DC₅₀s of 10 nM and 180 nM in H3122 cell and Karpas 299, respectively^[1].
TL13-12 (0-160 nM; 16 hours) degrades ALK and aurora A protein expression as a dose-dependent manner in Kelly and CHLA20 cells^[1].
TL13-12 (100 nM; 16 hours) significantly inhibits Tariqudan-induced ALK and Aurora A protein expression in CHLA20 cells^[1].

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

961.48

C₄₅H₅₃ClN₁₀O₁₀S

2229037-04-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Powell CE, et al. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).J Med Chem. 2018 May 10;61(9):4249-4255.