c-ABL-IN-3

发表于2023年11月22日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

c-ABL-IN-3

c-ABL-IN-3 是一种有效的 c-Abl 抑制剂。c-Abl 的激活与多种疾病有关，尤其是癌症。c-ABL-IN-3 具有研究神经退行性疾病（肌萎缩侧索硬化症 (ALS) 和帕金森病 (PD) 和癌症的潜力) (摘自专利 WO2021048567A1，化合物 50)。

c-ABL-IN-3 Chemical Structure

CAS No. : 2626934-64-1

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生物活性	c-ABL-IN-3 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-3 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 50)^[1].
分子量	376.29
Formula	C₁₇H₁₁F₃N₄O₃
CAS 号	2626934-64-1
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]. Michael J. RAWLING, et al. New compounds and methods. Patent WO2021048567A1.

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CHMFL-ABL-121

发表于2023年11月7日由上海金畔生物科技有限公司

CHMFL-ABL-121

CHMFL-ABL-121 是一种 II 型 ABL 激酶高效抑制剂，抑制纯化的非活性 ABL wt 和 T315I 激酶蛋白的 IC₅₀ 值分别为 2 nM 和 0.2 nM。

CHMFL-ABL-121 Chemical Structure

CAS No. : 2270879-07-5

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生物活性

CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC₅₀s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively^[1].

IC₅₀ & Target^[1]

ABL wt

2 nM (IC₅₀)

ABL-T315I

0.2 nM (IC₅₀)

体外研究
(In Vitro)

CHMFL-ABL-121 dose-dependently inhibits BCRABL’s auto-phosphorylation at Y245 site in K562 (EC₅₀<10 nm), meg-01 (ec₅₀<10 nm) and ku812 (ec₅₀<30 nm) cells and also significantly blocks the phosphorylation of downstream signaling mediators stat5, crkl erk^[1].
CHMFL-ABL-121 induces apoptosis and arrests cell cycle at G0/G1 phase^[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.

分子量

580.67

Formula

C₃₀H₃₁F₃N₆OS

CAS 号

2270879-07-5

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]. Liu X, et al. Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia. Eur J Med Chem. 2018 Dec 5;160:61-81.

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SNIPER(ABL)-058

发表于2023年11月7日由上海金畔生物科技有限公司

SNIPER(ABL)-058

SNIPER(ABL)-058，由 Imatinib (ABL 抑制剂) 通过 linker 与 LCL161 衍生物 (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 10 μM。

SNIPER(ABL)-058 Chemical Structure

CAS No. : 2222354-61-0

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生物活性	SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 10 μM^[1].
分子量	1150.39
Formula	C₆₂H₇₅N₁₁O₉S
CAS 号	2222354-61-0
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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SNIPER(ABL)-024

发表于2023年11月7日由上海金畔生物科技有限公司

SNIPER(ABL)-024

SNIPER(ABL)-024，由 GNF5 (ABL 抑制剂) 通过 linker 与 LCL161 衍生物 (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 5μM。

SNIPER(ABL)-024 Chemical Structure

CAS No. : 2222355-77-1

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生物活性	SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 5μM^[1].
分子量	1031.15
Formula	C₅₂H₆₁F₃N₈O₉S
CAS 号	2222355-77-1
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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SNIPER(ABL)-015

发表于2023年11月7日由上海金畔生物科技有限公司

SNIPER(ABL)-015

SNIPER(ABL)-015，由 GNF5 (ABL 抑制剂) 通过 linker 与 MV-1 (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 5μM。

SNIPER(ABL)-015 Chemical Structure

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生物活性	SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 5 μM ^[1].
分子量	1094.23
Formula	C₅₈H₇₀F₃N₉O₉
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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SNIPER(ABL)-050

发表于2023年11月7日由上海金畔生物科技有限公司

SNIPER(ABL)-050

SNIPER(ABL)-050，由 Imatinib (ABL 抑制剂) 通过 linker 与 MV-1 (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白。

SNIPER(ABL)-050 Chemical Structure

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生物活性	SNIPER(ABL)-050, conjugating Imatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein^[1].
分子量	1213.47
Formula	C₆₈H₈₄N₁₂O₉
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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SNIPER(ABL)-033

发表于2023年11月7日由上海金畔生物科技有限公司

SNIPER(ABL)-033

SNIPER(ABL)-033，由 HG-7-85-01 (ABL 抑制剂) 通过 linker 与 LCL161 衍生物 (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 0.3 μM。

SNIPER(ABL)-033 Chemical Structure

CAS No. : 2222354-18-7

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生物活性	SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 0.3 μM^[1].
分子量	1211.42
Formula	C₆₁H₇₃F₃N₁₀O₉S₂
CAS 号	2222354-18-7
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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SNIPER(ABL)-013

发表于2023年11月7日由上海金畔生物科技有限公司

SNIPER(ABL)-013

SNIPER(ABL)-013，由 GNF5 (ABL 抑制剂) 通过 linker 与 Bestatin (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 20 μM。

SNIPER(ABL)-013 Chemical Structure

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生物活性	SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 20 μM^[1].
分子量	839.90
Formula	C₄₂H₅₂F₃N₇O₈
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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SNIPER(ABL)-019

发表于2023年11月7日由上海金畔生物科技有限公司

SNIPER(ABL)-019

SNIPER(ABL)-019，由 Dasatinib (ABL 抑制剂) 通过 linker 与 MV-1 (cIAP1 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 0.3 μM。

SNIPER(ABL)-019 Chemical Structure

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生物活性	SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 0.3 μM^[1].
分子量	1177.85
Formula	C₆₀H₇₇ClN₁₂O₉S
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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SNIPER(ABL)-044

发表于2023年11月7日由上海金畔生物科技有限公司

SNIPER(ABL)-044

SNIPER(ABL)-044，由 HG-7-85-01 (ABL 抑制剂) 通过 linker 与 Bestatin (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 10 μM。

SNIPER(ABL)-044 Chemical Structure

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生物活性	SNIPER(ABL)-044, conjugating HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 10 μM^[1].
分子量	1020.17
Formula	C₅₁H₆₄F₃N₉O₈S
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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SNIPER(ABL)-049

发表于2023年11月7日由上海金畔生物科技有限公司

SNIPER(ABL)-049

SNIPER(ABL)-049，由 Imatinib (ABL 抑制剂) 通过 linker 与 Bestatin (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 100 μM。

SNIPER(ABL)-049 Chemical Structure

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生物活性	SNIPER(ABL)-049, conjugating Imatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 100 μM^[1].
分子量	959.14
Formula	C₅₂H₆₆N₁₀O₈
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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BCR-ABL-IN-1

发表于2023年11月6日由上海金畔生物科技有限公司

BCR-ABL-IN-1

BCR-ABL-IN-1 是一种 BCR-ABL 酪氨酸激酶抑制剂，pIC₅₀ 值为 6.46，可能用于慢性髓细胞白血病的研究。

BCR-ABL-IN-1 Chemical Structure

CAS No. : 188260-50-6

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生物活性	BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC₅₀ of 6.46, and may be used in the research of chronic myelogenous leukemia.
IC₅₀ & Target	pIC50: 6.46 (BCR-ABL)^[1]
体外研究 (In Vitro)	BCR-ABL-IN-1 (Compound 21) is an inhibitor of BCR-ABL tyrosine kinase, with a pIC₅₀ of 6.46, and may be used in the research of chronic myelogenous leukemia. 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.
分子量	459.44
Formula	C₂₃H₂₁F₄N₅O
CAS 号	188260-50-6
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]. Cui J1, et al. BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2442-50.

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BCR-ABL-IN-2

发表于2023年11月6日由上海金畔生物科技有限公司

BCR-ABL-IN-2

BCR-ABL-IN-2 是 BCR-ABL1 激酶的抑制剂，其对 ABL1^native 和 ABL1^T315I 的 IC₅₀ 值分别为 57 nM，773 nM。

BCR-ABL-IN-2 Chemical Structure

CAS No. : 897369-18-5

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生物活性	BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC₅₀s of 57 nM, 773 nm for ABL1^native and ABL1^T315I, respectively.
IC₅₀ & Target	IC50: 57 nM (ABL1^native), 773 nM (ABL1^T315I)^[1].
体外研究 (In Vitro)	BCR-ABL-IN-2 (Compound 1) contains a urea moiety to allow a hydrogen bond with the conserved K271-E286 salt bridge of ABL1, a t-butyl moiety to bind into the hydrophobic spine at the third pocket position, and a 2,3-dichlorophenyl ring to stabilize the DFG-phenylalanine F382 in the Type II-out conformation. BCR-ABL-IN-2 exhibits an IC₅₀ of 57 nM for ABL1^native and an IC₅₀ of 773 nM for ABL1^T315I^[1]. Despite ABL, BCR-ABL-IN-2 can also inhibit KDR, BRaf, p38 kinase with IC₅₀s of 1.8 μM, 0.23 μM, 6.3 nM, 43 nM, respectively^[2]. 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.
分子量	502.39
Formula	C₂₄H₂₅Cl₂N₅O₃
CAS 号	897369-18-5
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]. Chan WW, et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell. 2011 Apr 12;19(4):556-68. [2]. ARYL SULFONOHYDRAZIDES. US 2008/0113967 A1.

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SNIPER(ABL)-039

发表于2023年11月6日由上海金畔生物科技有限公司

SNIPER(ABL)-039

SNIPER(ABL)-039，由 Dasatinib (ABL 抑制剂) 通过 linker 与 LCL161 衍生物 (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 10 nM。对 ABL，cIAP1，cIAP2，XIAP 的 IC₅₀ 分别为 0.54 nM，10 nM，12 nM 和 50 nM。

SNIPER(ABL)-039 Chemical Structure

CAS No. : 2222354-29-0

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生物活性

SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 10 nM. IC₅₀s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively^[1].

IC₅₀ & Target^[1]

Abl

0.54 nM (IC₅₀)

cIAP1

10 nM (IC₅₀)

cIAP2

12 nM (IC₅₀)

XIAP

50 nM (IC₅₀)

SNIPER

Abl

10 nM (DC₅₀)

分子量

1114.77

Formula

C₅₄H₆₈ClN₁₁O₉S₂

CAS 号

2222354-29-0

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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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SNIPER(ABL)-047

发表于2023年11月6日由上海金畔生物科技有限公司

SNIPER(ABL)-047

SNIPER(ABL)-047，由 HG-7-85-01 (ABL 抑制剂) 通过 linker 与 MV-1 (IAP 配体) 组合而成，可有效降解 BCR-ABL 蛋白，DC₅₀ 为 2 μM。

SNIPER(ABL)-047 Chemical Structure

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生物活性	SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 2 μM^[1].
分子量	1274.50
Formula	C₆₇H₈₂F₃N₁₁O₉S
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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DPH

发表于2023年11月3日由上海金畔生物科技有限公司

DPH 纯度: 99.20%

DPH 是一种有效的，细胞渗透的 c-Abl 激活剂，在酶和细胞活动中，能够有效刺激 c-Abl 的活化。

DPH Chemical Structure

CAS No. : 484049-04-9

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10 mM * 1 mL in DMSO	￥1249	In-stock
10 mg	￥1135	In-stock
50 mg	￥4557	In-stock
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DPH 相关产品

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生物活性

DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.

体外研究
(In Vitro)

DPH binds to the myristoyl binding site and prevents the formation of the bent conformation of the αI helix through steric hindrance, a mode of action distinct from the previously identified allosteric c-Abl inhibitor, GNF-2, that also binds to the myristoyl binding site. DPH represents the first cell-permeable, small-molecule tool compound for c-Abl activation^[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.

分子量

336.32

Formula

C₁₈H₁₃FN₄O₂

CAS 号

484049-04-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (297.34 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9734 mL	14.8668 mL	29.7336 mL
5 mM	0.5947 mL	2.9734 mL	5.9467 mL
10 mM	0.2973 mL	1.4867 mL	2.9734 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。-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： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.43 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (7.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.43 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (7.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.43 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Yang J, et al. Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site. Chem Biol. 2011 Feb 25;18(2):177-86

[2]. Shapiro LP, et al. Corticosteroid-induced dendrite loss and behavioral deficiencies can be blocked by activation of Abl2/Arg kinase. Mol Cell Neurosci. 2017 Oct 26;85:226-234.

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Asciminib(Synonyms: ABL001)

发表于2023年9月9日由上海金畔生物科技有限公司

Asciminib (Synonyms: ABL001) 纯度: 99.78%

Asciminib (ABL001) 是一种有效和选择性的变构 BCR-ABL1 抑制剂，抑制 Ba/F3 细胞生长的 IC₅₀ 值为 0.25 nM。

Asciminib Chemical Structure

CAS No. : 1492952-76-7

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1700	In-stock
5 mg	￥1550	In-stock
10 mg	￥2450	In-stock
50 mg	￥5500	In-stock
100 mg	￥9500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Asciminib 相关产品

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Rare Diseases Drug Library

生物活性

Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC₅₀ of 0.25 nM^[1].

体外研究
(In Vitro)

Asciminib binds to the myristoyl pocket of ABL1 and induces the formation of an inactive kinase conformation. NMR and biophysical studies confirm that asciminib binds potently (dissociation constant=0.5-0.8nM) and selectively to the myristoyl pocket of ABL1 and induces the inactive C-terminal helix conformation. Asciminib binding mimics the structural consequences of myristate binding to the N terminus of ABL1. Consistent with this binding site, asciminib exhibits the same non-ATP-competitive biochemical kinetics as the BCR–ABL inhibitor GNF-2 but with approximately 100-fold greater potency. Asciminib lacks activity against more than 60 kinases, including SRC, and is similarly inactive against G-protein-coupled receptors, ion channels, nuclear receptors and transporters. In BCR–ABL1-transformed Ba/F3 cells grown without IL-3, asciminib has an anti-proliferative with IC₅₀ value of 0.25nM. In the CML blast-phase cell line KCL-22, asciminib inhibits phosphorylation of both STAT5 (Tyr694; pSTAT5) and BCR–ABL1 (Tyr245; pBCR–ABL1) after 1h using concentrations that correlate with those required for inhibition of cell proliferation. Asciminib is selectively active against all BCR–ABL1 lines (IC₅₀ value of 1–20nM), irrespective of the presence of either the p210 or the p190 BCR–ABL1 isoform.^[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.

体内研究
(In Vivo)

Asciminib is undergoing clinical development testing in patients with CML and Philadelphia chromosome-positive acute lymphoblastic leukaemia. Single doses of 7.5, 15 and 30 mg/kg ABL001, administered to mice bearing KCL- 22 xenografts, inhibits pSTAT5 (Tyr694), which return to baseline at 10, 12 and 16-20h after administration of the dose, respectively. In mice implanted with KCL-22 tumors, the minimum dose of asciminib required for complete regression is 7.5 mg/kg twice a day (BID) or 30 mg/kg once a day (QD), and is tolerated at doses up to 250 mg/kg BID. Similarly, in xenografts derived from patients, treatment with 7.5 and 30 mg/kg asciminib leads to regressions that are maintained during dosing^[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

449.84

Formula

C₂₀H₁₈ClF₂N₅O₃

CAS 号

1492952-76-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (222.30 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2230 mL	11.1151 mL	22.2301 mL
5 mM	0.4446 mL	2.2230 mL	4.4460 mL
10 mM	0.2223 mL	1.1115 mL	2.2230 mL

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：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.56 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.56 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.56 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Wylie AA, et al. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1. Nature. 2017 Mar 30;543(7647):733-737.

Cell Assay ^[1]	Ba/F3 cells are treated with a range concentration of asciminib (0-10000 nM) for 48 h. Cell proliferation is measured using the Britelite luciferase detection assay^[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 Administration ^[1]	Mice: Asciminib efficacy in three patient-derived ALL systemic xenograft models (ALL-7015, AL-7119 and AL-7155) is assessed by FACS monitoring of the percentage of CD45+ cells per live cell in blood samples taken at varying time points after dosing with either 7.5 mg/kg BID (group 2) or 30 mg/kg BID (group 3) asciminib for 3 weeks^[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.
参考文献	[1]. Wylie AA, et al. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1. Nature. 2017 Mar 30;543(7647):733-737.

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BCR-ABL-IN-3

发表于2023年8月26日由上海金畔生物科技有限公司

BCR-ABL-IN-3

BCR-ABL-IN-3 是一种有效且不可逆的 Bcr-Abl 抑制剂，对于 Ba/F₃Bcr-Abl^T3151 的 IC₅₀ 为 ≤100 nM。BCR-ABL-IN-3 具有抗癌活性。

BCR-ABL-IN-3 Chemical Structure

CAS No. : 2240191-12-0

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

BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor with an IC₅₀ of ≤100 nM for Ba/F₃Bcr-Abl^T3151. BCR-ABL-IN-3 has anti-cancer activity^[1].

IC₅₀ & Target^[1]

Ba/F₃Bcr-Abl^T3151

≤100 nM (IC₅₀)

体内研究
(In Vivo)

BCR-ABL-IN-3 (compound 7; 15 mg/kg; twice a day; for 19 days) has good antitumor effect in female NOD/SCID mice of 7-8 weeks weighing 21.8 g with Ba/F₃Bcr-Abl^T3151 cells^[1].
BCR-ABL-IN-3 (2 mg/kg for IV or 20mg/kg for PO) has a C_max of 5485 ng/mL and an AUC of 5450 h•ng/mL for IV in male Sprague Dawley rats of 7-8 weeks old weighing 210 g^[1].

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

分子量

466.89

Formula

C₂₀H₁₇ClF₂N₄O₃S

CAS 号

2240191-12-0

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]. Hanyi Wang, et al. (hetero)arylamide compound for inhibiting protein kinase activity. WO2018133826A1.

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CHMFL-ABL/KIT-155(Synonyms: CHMFL-ABL-KIT-155)

发表于2023年8月20日由上海金畔生物科技有限公司

CHMFL-ABL/KIT-155 (Synonyms: CHMFL-ABL-KIT-155)

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) 是一种高效的，具有口服活性的 type II ABL/c-KIT 双激酶抑制剂 (IC₅₀ 分别为 46 nM 和 75 nM)，对 BLK (IC₅₀=81 nM), CSF1R (IC₅₀=227 nM), DDR1 (IC₅₀=116 nM), DDR2 (IC₅₀=325 nM), LCK (IC₅₀=12 nM), PDGFRβ (IC₅₀=80 nM) 激酶也具有明显的抑制活性。CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) 阻止细胞周期进展和诱导细胞凋亡。

CHMFL-ABL/KIT-155 Chemical Structure

CAS No. : 2081093-21-0

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	CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC₅₀s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC₅₀=81 nM), CSF1R (IC₅₀=227 nM), DDR1 (IC₅₀=116 nM), DDR2 (IC₅₀=325 nM), LCK (IC₅₀=12 nM) and PDGFRβ (IC₅₀=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis^[1].
IC₅₀ & Target	IC50: 46 nM (type II ABL), 75 nM (c-KIT), 81 nM (BLK), 227 nM (CSF1R), 116 nM (DDR1), 325 nM (DDR2), 12 nM (LCK), 80 nM (PDGFRβ)^[1]
体外研究 (In Vitro)	CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) exhibits anti-proliferation activities in the BCR-ABL dependent CML cancer cell lines such as K562 (GI₅₀: 0.027 µM), MEG-01 (GI₅₀: 0.02 µM), and KU812 (GI₅₀: 0.056 µM). It also potently inhibits the growth of c-KIT dependent GISTs cancer cell lines including GIST-T1 (GI₅₀: 0.023 µM), GIST-882 (GI₅₀: 0.095 µM) but not c-KIT independent GIST-48B (GI₅₀: 3.96 µM) ^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)	CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) (25-100 mg/kg; p.o.; once daily for 28 days) shows dose-dependent tumor progression suppression without apparent toxicity in female nu/nu mice bearing established K562 tumor xenografts^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	609.68
Formula	C₃₃H₃₈F₃N₅O₃
CAS 号	2081093-21-0
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]. Wang Q, et al. Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. J Med Chem. 2017 Jan 12;60(1):273-289.

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多肽定制Abl Cytosolic Substrate 编码

发表于2023年7月8日由上海金畔生物科技有限公司

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称	Abl Cytosolic Substrate
编码
别名	Abl Cytosolic Substrate
纯度	80%，90%，95%，98%，99%
重量	1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写）	EAIYAAPFAKKK
序列（三字母缩写）	Glu-Ala-Ile-Tyr-Ala-Ala-Pro-Phe-Ala-Lys-Lys-Lys
基本描述
溶解度
分子量	1336.61
化学式	C64H101N15O16
存储条件	Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
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标签归档：abl

c-ABL-IN-3

CHMFL-ABL-121

SNIPER(ABL)-058

SNIPER(ABL)-024

SNIPER(ABL)-015

SNIPER(ABL)-050

SNIPER(ABL)-033

SNIPER(ABL)-013

SNIPER(ABL)-019

SNIPER(ABL)-044

SNIPER(ABL)-049

BCR-ABL-IN-1

BCR-ABL-IN-2

SNIPER(ABL)-039

SNIPER(ABL)-047

DPH

DPH 相关产品

•相关化合物库:

Asciminib(Synonyms: ABL001)

Asciminib 相关产品

•相关化合物库:

BCR-ABL-IN-3

CHMFL-ABL/KIT-155(Synonyms: CHMFL-ABL-KIT-155)

多肽定制Abl Cytosolic Substrate 编码