BTK-IN-11 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-11 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022063101A1, compound Z2)[1].
分子量
487.94
Formula
C26H22ClN5O3
CAS 号
2765852-46-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Fusheng Zhou, et al. Aroyl substituted tricyclic compound, preparation method therefor and use thereof. Patent WO2022063101A1.
BTK-IN-14 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-14 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022057894A1, compound 1)[1].
分子量
676.81
Formula
C38H44N8O4
CAS 号
2764674-60-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Guangxiu Dai, et al. Heteroaryl heterocyclic compounds and uses thereof. Patent WO2022057894A1.
BTK-IN-12 is a potent BTK inhibitor with IC50s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8)[1].
分子量
505.54
Formula
C27H28FN5O4
CAS 号
2762043-53-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Xiangyang Chen, et al. Heterocyclic compounds as btk inhibitors. WO2022037649A1.
BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels(ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity[1].
体外研究 (In Vitro)
BTK-IN-7 (compound 24a; 10, 100, 1000, 10000 nM; 48 hours) displays the antiproliferative effects in U-937 cells (IC50=3.6 μM)[1]. BTK-IN-7 (10, 100, 1000, 10000 nM; 48 hours; U937 cells) induces cell cycle arrest at the G1 phase in a concentration-dependent manner[1]. BTK-IN-7 (1-5 μM; 48 hours) induces apoptosis in U-937 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
Cell Line:
U937, Ramos, Pfeiffer, Jeko-1 cells
Concentration:
10, 100, 1000, 10000 nM
Incubation Time:
48 hours
Result:
Displayed antiproliferative effects in U-937 (IC50=3.6 μM) cells.
Cell Cycle Analysis[1]
Cell Line:
U937 cells
Concentration:
10, 100, 1000, 10000 nM
Incubation Time:
48 hours
Result:
Cells were arrested atthe G1 phase in a concentration-dependent manner.
Apoptosis Analysis[1]
Cell Line:
U937 cells
Concentration:
1, 2.5, 5 μM
Incubation Time:
48 hours
Result:
An apoptosis rate was increased to 22.75% at a concentration of 5 μM.
体内研究 (In Vivo)
BTK-IN-7 (25 and 50 mg/kg; intraperitoneal injection; daily for 14 days) inhibits tumor growth in a dose-dependent manner in U-937 xenograft mouse model, and 50 mg/kg dosage displays a better antitumor effect. BTK-IN-7 does not show significant parenchymal injury or inflammatory cell infiltration in organs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male BALB/c nude mice (U397 xenograft mouse model) [1]
Dosage:
25, 50 mg/kg
Administration:
Intraperitoneal injection; daily for 14 days
Result:
Inhibited tumor growth in a dose-dependent manner and did not reveal significant parenchymal injury or inflammatory cell infiltration in organs.
分子量
540.61
Formula
C30H32N6O4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Dou D, et al. Discovery of Pteridine-7(8H)-one Derivatives as Potent and Selective Inhibitors of Bruton’s Tyrosine Kinase (BTK). J Med Chem. 2022;65(3):2694-2709.
BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels(ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity[1].
体外研究 (In Vitro)
BTK-IN-7 (compound 24a; 10, 100, 1000, 10000 nM; 48 hours) displays the antiproliferative effects in U-937 cells (IC50=3.6 μM)[1]. BTK-IN-7 (10, 100, 1000, 10000 nM; 48 hours; U937 cells) induces cell cycle arrest at the G1 phase in a concentration-dependent manner[1]. BTK-IN-7 (1-5 μM; 48 hours) induces apoptosis in U-937 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
Cell Line:
U937, Ramos, Pfeiffer, Jeko-1 cells
Concentration:
10, 100, 1000, 10000 nM
Incubation Time:
48 hours
Result:
Displayed antiproliferative effects in U-937 (IC50=3.6 μM) cells.
Cell Cycle Analysis[1]
Cell Line:
U937 cells
Concentration:
10, 100, 1000, 10000 nM
Incubation Time:
48 hours
Result:
Cells were arrested atthe G1 phase in a concentration-dependent manner.
Apoptosis Analysis[1]
Cell Line:
U937 cells
Concentration:
1, 2.5, 5 μM
Incubation Time:
48 hours
Result:
An apoptosis rate was increased to 22.75% at a concentration of 5 μM.
体内研究 (In Vivo)
BTK-IN-7 (25 and 50 mg/kg; intraperitoneal injection; daily for 14 days) inhibits tumor growth in a dose-dependent manner in U-937 xenograft mouse model, and 50 mg/kg dosage displays a better antitumor effect. BTK-IN-7 does not show significant parenchymal injury or inflammatory cell infiltration in organs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male BALB/c nude mice (U397 xenograft mouse model) [1]
Dosage:
25, 50 mg/kg
Administration:
Intraperitoneal injection; daily for 14 days
Result:
Inhibited tumor growth in a dose-dependent manner and did not reveal significant parenchymal injury or inflammatory cell infiltration in organs.
分子量
540.61
Formula
C30H32N6O4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Dou D, et al. Discovery of Pteridine-7(8H)-one Derivatives as Potent and Selective Inhibitors of Bruton’s Tyrosine Kinase (BTK). J Med Chem. 2022;65(3):2694-2709.
BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels(ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity[1].
体外研究 (In Vitro)
BTK-IN-7 (compound 24a; 10, 100, 1000, 10000 nM; 48 hours) displays the antiproliferative effects in U-937 cells (IC50=3.6 μM)[1]. BTK-IN-7 (10, 100, 1000, 10000 nM; 48 hours; U937 cells) induces cell cycle arrest at the G1 phase in a concentration-dependent manner[1]. BTK-IN-7 (1-5 μM; 48 hours) induces apoptosis in U-937 cells[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.
Cell Proliferation Assay[1]
Cell Line:
U937, Ramos, Pfeiffer, Jeko-1 cells
Concentration:
10, 100, 1000, 10000 nM
Incubation Time:
48 hours
Result:
Displayed antiproliferative effects in U-937 (IC50=3.6 μM) cells.
Cell Cycle Analysis[1]
Cell Line:
U937 cells
Concentration:
10, 100, 1000, 10000 nM
Incubation Time:
48 hours
Result:
Cells were arrested atthe G1 phase in a concentration-dependent manner.
Apoptosis Analysis[1]
Cell Line:
U937 cells
Concentration:
1, 2.5, 5 μM
Incubation Time:
48 hours
Result:
An apoptosis rate was increased to 22.75% at a concentration of 5 μM.
体内研究 (In Vivo)
BTK-IN-7 (25 and 50 mg/kg; intraperitoneal injection; daily for 14 days) inhibits tumor growth in a dose-dependent manner in U-937 xenograft mouse model, and 50 mg/kg dosage displays a better antitumor effect. BTK-IN-7 does not show significant parenchymal injury or inflammatory cell infiltration in organs[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.
Animal Model:
Male BALB/c nude mice (U397 xenograft mouse model) [1]
Dosage:
25, 50 mg/kg
Administration:
Intraperitoneal injection; daily for 14 days
Result:
Inhibited tumor growth in a dose-dependent manner and did not reveal significant parenchymal injury or inflammatory cell infiltration in organs.
分子量
540.61
Formula
C30H32N6O4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Dou D, et al. Discovery of Pteridine-7(8H)-one Derivatives as Potent and Selective Inhibitors of Bruton’s Tyrosine Kinase (BTK). J Med Chem. 2022;65(3):2694-2709.
BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells[1].
分子量
481.46
Formula
C25H19N7O4
CAS 号
2361192-21-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Ran F, et al. Design and synthesis of novel pyrazolopyrimidine-based derivatives as reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. Med Chem Res, 2022, 31, 594-604.
BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells[1].
分子量
481.46
Formula
C25H19N7O4
CAS 号
2361192-21-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Ran F, et al. Design and synthesis of novel pyrazolopyrimidine-based derivatives as reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. Med Chem Res, 2022, 31, 594-604.
BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells[1].
分子量
481.46
Formula
C25H19N7O4
CAS 号
2361192-21-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Ran F, et al. Design and synthesis of novel pyrazolopyrimidine-based derivatives as reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. Med Chem Res, 2022, 31, 594-604.
BTK-IN-6 是布鲁顿酪氨酸激酶 (BTK) 的有效抑制剂。BTK 是 Tec 酪氨酸激酶家族的成员，在调节早期 B 细胞发育和成熟 B 细胞活化和存活中起重要作用。BTK-IN-6 具有研究免疫疾病、癌症、心血管疾病、病毒感染、炎症、代谢/内分泌功能障碍和神经系统疾病的潜力 (摘自专利 WO2021136219A1，化合物 8)。
BTK-IN-6 Chemical Structure
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
BTK-IN-6 is a potent inhibitor of Bruton’s Tyrosine Kinase (BTK). BTK is a member of the Tec family of tyrosine kinases and plays an important role in the regulation of early B-cell development and mature B-cell activation and survival. BTK-IN-6 has the potential for the research of immune disorders, cancer, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders, and neurological disorders (extracted from patent WO2021136219A1, compound 8)[1].
分子量
435.45
Formula
C23H22FN5O3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Quan Zhou, et al. Btk inhibitors. Patent WO2021136219A1.
BTK-IN-6 是布鲁顿酪氨酸激酶 (BTK) 的有效抑制剂。BTK 是 Tec 酪氨酸激酶家族的成员，在调节早期 B 细胞发育和成熟 B 细胞活化和存活中起重要作用。BTK-IN-6 具有研究免疫疾病、癌症、心血管疾病、病毒感染、炎症、代谢/内分泌功能障碍和神经系统疾病的潜力 (摘自专利 WO2021136219A1，化合物 8)。
BTK-IN-6 Chemical Structure
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
BTK-IN-6 is a potent inhibitor of Bruton’s Tyrosine Kinase (BTK). BTK is a member of the Tec family of tyrosine kinases and plays an important role in the regulation of early B-cell development and mature B-cell activation and survival. BTK-IN-6 has the potential for the research of immune disorders, cancer, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders, and neurological disorders (extracted from patent WO2021136219A1, compound 8)[1].
分子量
435.45
Formula
C23H22FN5O3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Quan Zhou, et al. Btk inhibitors. Patent WO2021136219A1.
BTK-IN-6 是布鲁顿酪氨酸激酶 (BTK) 的有效抑制剂。BTK 是 Tec 酪氨酸激酶家族的成员，在调节早期 B 细胞发育和成熟 B 细胞活化和存活中起重要作用。BTK-IN-6 具有研究免疫疾病、癌症、心血管疾病、病毒感染、炎症、代谢/内分泌功能障碍和神经系统疾病的潜力 (摘自专利 WO2021136219A1，化合物 8)。
BTK-IN-6 Chemical Structure
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
BTK-IN-6 is a potent inhibitor of Bruton’s Tyrosine Kinase (BTK). BTK is a member of the Tec family of tyrosine kinases and plays an important role in the regulation of early B-cell development and mature B-cell activation and survival. BTK-IN-6 has the potential for the research of immune disorders, cancer, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders, and neurological disorders (extracted from patent WO2021136219A1, compound 8)[1].
分子量
435.45
Formula
C23H22FN5O3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Quan Zhou, et al. Btk inhibitors. Patent WO2021136219A1.
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM[1].
体外研究 (In Vitro)
Pirtobrutinib potently inhibits both wild-type BTK and BTK C481S-mediated kinase activity with nanomolar potency. Pirtobrutinib inhibits WT BTK (Y223) autophosphorylation with an IC50 of 3.68 nM. Pirtobrutinib inhibits BTK C481S Y223, C481T Y223, and C481R Y223 autophosphorylation with IC50s of 8.45, 7.23, and 11.73 nM, 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.
Clinical Trial
分子量
479.43
Formula
C22H21F4N5O3
CAS 号
2101700-15-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Gomez E B , et al. Loxo-305, a Highly Selective and Non-Covalent Next Generation BTK Inhibitor, Inhibits Diverse BTK C481 Substitution Mutations[J]. Blood, 2019, 134(Supplement_1):4644-4644.
