1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. (Rac)-JBJ-04-125-02

(Rac)-JBJ-04-125-02 是 JBJ-04-125-02 的消旋体。JBJ-04-125-02 是一种有效的,选择性突变,变构和口服活性的 EGFR 抑制剂。

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(Rac)-JBJ-04-125-02

(Rac)-JBJ-04-125-02 Chemical Structure

CAS No. : 2140807-05-0

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1 mg ¥1066
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5 mg ¥2800
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10 mg ¥4500
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(Rac)-JBJ-04-125-02 的其他形式现货产品:

Customer Review

Other Forms of (Rac)-JBJ-04-125-02:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor[1].

IC50 & Target[1]

EGFR (L858R/T790M)

0.26 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
0.1 μM
Compound: 2; JBJ-04-125-02
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by MTS assay
[PMID: 36279692]
BaF3 IC50
0.1 μM
Compound: 6; JBJ-04-125-02
Antiproliferative activity against mouse BaF3 cells stably transfected with EGFR L858R/T790M/C797S (unknown origin) assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells stably transfected with EGFR L858R/T790M/C797S (unknown origin) assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
[PMID: 33243531]
BaF3 IC50
1550 nM
Compound: 6; JBJ-04-125-02
Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/C797S mutant assessed as reduction in cell viability measured after 72 hrs by cell titre glo luminescence assay
Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/C797S mutant assessed as reduction in cell viability measured after 72 hrs by cell titre glo luminescence assay
[PMID: 36178776]
BaF3 IC50
30 nM
Compound: 6; JBJ-04-125-02
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability measured after 72 hrs by cell titre glo luminescence assay
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability measured after 72 hrs by cell titre glo luminescence assay
[PMID: 36178776]
Sf9 IC50
73.1 nM
Compound: 2b; JBJ-04-125-02
Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA
Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA
[PMID: 31298540]
体外研究
(In Vitro)

JBJ-04-125-02 是一种有效的突变选择性变构和具有口服活性的 EGFR 抑制剂,对 EGFRL858R/T790M 的 IC50 为 0.26 nM[1]

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

分子量

543.61

Formula

C29H26FN5O3S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
(Rac)-JBJ-04-125-02
目录号:
HY-135805A
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