JTE-952

目录号: HY-122906 纯度: 99.95%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

JTE-952 是集落刺激因子-1 受体 (CSF-1R/cFMS) 有效的、具有口服活性的、 II 型选择性抑制剂，其对 CSF1R 和 TrkA 的IC₅₀ 值分别为 13 nM 和 261 nM。可用于关节炎的相关研究。

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JTE-952 Chemical Structure

CAS No. : 1255303-54-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4560	In-stock
1 mg	￥1600	In-stock
5 mg	￥4000	In-stock
10 mg	现货	询价
50 mg		询价
100 mg		询价

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生物活性
纯度 & 产品资料
参考文献

生物活性

JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC₅₀ values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis^[1].

IC₅₀ & Target

IC50: 13 nM (CSF1R), 261 nM (TrkA)^[1].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal GST-tagged FGFR1 (456 to 765 residues) expressed in baculovirus infected Sf21 insect cells using IGF-IRtide (12-527) as substrate Inhibition of human N-terminal GST-tagged FGFR1 (456 to 765 residues) expressed in baculovirus infected Sf21 insect cells using IGF-IRtide (12-527) as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal GST-tagged EGFR (696 to end residues) expressed in baculovirus infected Sf21 insect cells using Angiotensin II peptide as substrate Inhibition of human N-terminal GST-tagged EGFR (696 to end residues) expressed in baculovirus infected Sf21 insect cells using Angiotensin II peptide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His-tagged JNK1alpha1 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate Inhibition of human N-terminal His-tagged JNK1alpha1 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of recombinant human N-terminal His6-tagged Abl (27 to end residues) expressed in baculovirus infected Sf21 insect cells using Abltide as substrate Inhibition of recombinant human N-terminal His6-tagged Abl (27 to end residues) expressed in baculovirus infected Sf21 insect cells using Abltide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of recombinant full-length human N-terminal His6-tagged AuroraA expressed in baculovirus infected Sf21 insect cells using Kemptide as substrate Inhibition of recombinant full-length human N-terminal His6-tagged AuroraA expressed in baculovirus infected Sf21 insect cells using Kemptide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of recombinant full-length human N-terminal GST-tagged CDK1/cyclinB expressed in baculovirus infected Sf21 insect cells using Abltide as substrate Inhibition of recombinant full-length human N-terminal GST-tagged CDK1/cyclinB expressed in baculovirus infected Sf21 insect cells using Abltide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full length C-terminal His6-tagged Cdk2/human full length N-terminal GST-tagged Cyclin A expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate Inhibition of human full length C-terminal His6-tagged Cdk2/human full length N-terminal GST-tagged Cyclin A expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full length N-terminal GST-tagged CHK1 expressed in baculovirus infected Sf21 insect cells using CHKtide as substrate Inhibition of human full length N-terminal GST-tagged CHK1 expressed in baculovirus infected Sf21 insect cells using CHKtide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full length His6-tagged CK2alpha expressed in baculovirus infected Sf21 insect cells using Casein Kinase 2 substrate peptide Inhibition of human full length His6-tagged CK2alpha expressed in baculovirus infected Sf21 insect cells using Casein Kinase 2 substrate peptide	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal GST-tagged c-kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate Inhibition of human N-terminal GST-tagged c-kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged FGFR3 (447 to 761 residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate Inhibition of human N-terminal His6-tagged FGFR3 (447 to 761 residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal GST-tagged Flt1 (783 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate Inhibition of human N-terminal GST-tagged Flt1 (783 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal GST-tagged Flt3 (564 to end residues) expressed in baculovirus infected Sf21 insect cells using Abltide as substrate Inhibition of human N-terminal GST-tagged Flt3 (564 to end residues) expressed in baculovirus infected Sf21 insect cells using Abltide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full-length N-terminal His6-tagged Fyn expressed in baculovirus infected Sf21 insect cells using Src peptide as substrate Inhibition of human full-length N-terminal His6-tagged Fyn expressed in baculovirus infected Sf21 insect cells using Src peptide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 insect cells using phosphoglycogen synthase peptide-2 as substrate Inhibition of human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 insect cells using phosphoglycogen synthase peptide-2 as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of full-length human N-terminal His6-tagged IKKbeta expressed in baculovirus infected Sf21 insect cells using IKKtide as substrate Inhibition of full-length human N-terminal His6-tagged IKKbeta expressed in baculovirus infected Sf21 insect cells using IKKtide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of full-length human N-terminal His-tagged JNK2alpha2 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate Inhibition of full-length human N-terminal His-tagged JNK2alpha2 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of full-length human N-terminal His6-tagged JNK3 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate Inhibition of full-length human N-terminal His6-tagged JNK3 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His-tagged KDR (790 to end residues) expressed in baculovirus infected Sf21 insect cells using myelin basic protein as substrate Inhibition of human N-terminal His-tagged KDR (790 to end residues) expressed in baculovirus infected Sf21 insect cells using myelin basic protein as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of full-length human N-terminal His6-tagged LCK expressed in baculovirus infected Sf21 insect cells using Src peptide as substrate Inhibition of full-length human N-terminal His6-tagged LCK expressed in baculovirus infected Sf21 insect cells using Src peptide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of full-length human N-terminal His6-tagged LYN expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate Inhibition of full-length human N-terminal His6-tagged LYN expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged MET (974 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate Inhibition of human N-terminal His6-tagged MET (974 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged MSK1 (2 to end residues) expressed in baculovirus infected Sf21 insect cells using Crosstide as substrate Inhibition of human N-terminal His6-tagged MSK1 (2 to end residues) expressed in baculovirus infected Sf21 insect cells using Crosstide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full-length N-terminal His-tagged p70S6K expressed in baculovirus infected Sf21 insect cells using CKRRRLASLR as substrate Inhibition of human full-length N-terminal His-tagged p70S6K expressed in baculovirus infected Sf21 insect cells using CKRRRLASLR as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged PDGFRalpha (550 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate Inhibition of human N-terminal His6-tagged PDGFRalpha (550 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged PDGFRbeta (557 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate Inhibition of human N-terminal His6-tagged PDGFRbeta (557 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged PDK1 (52 to end residues) expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate Inhibition of human N-terminal His6-tagged PDK1 (52 to end residues) expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full-length N-terminal His6-tagged PKBalpha expressed in baculovirus infected Sf21 insect cells using Crosstide as substrate Inhibition of human full-length N-terminal His6-tagged PKBalpha expressed in baculovirus infected Sf21 insect cells using Crosstide as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full-length N-terminal His6-tagged PKCalpha expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate Inhibition of human full-length N-terminal His6-tagged PKCalpha expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged (2 to end residues) PKCbeta expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate Inhibition of human N-terminal His6-tagged (2 to end residues) PKCbeta expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full-length N-terminal His6-tagged PKCgamma expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate Inhibition of human full-length N-terminal His6-tagged PKCgamma expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged (11 to 552 residues) ROCK2 expressed in baculovirus infected Sf21 insect cells using Long S6 Kinase as substrate Inhibition of human N-terminal His6-tagged (11 to 552 residues) ROCK2 expressed in baculovirus infected Sf21 insect cells using Long S6 Kinase as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full-length N-terminal GST-tagged SAPK2a expressed in baculovirus infected Sf21 insect cells using MBP as substrate Inhibition of human full-length N-terminal GST-tagged SAPK2a expressed in baculovirus infected Sf21 insect cells using MBP as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full-length N-terminal GST-tagged SAPK2b2 expressed in baculovirus infected Sf21 insect cells using MBP as substrate Inhibition of human full-length N-terminal GST-tagged SAPK2b2 expressed in baculovirus infected Sf21 insect cells using MBP as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged SYK expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate Inhibition of human N-terminal His6-tagged SYK expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal His6-tagged TIE2 (771 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate Inhibition of human N-terminal His6-tagged TIE2 (771 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate	[PMID: 30755337]
Sf21	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full-length C-terminal His6-tagged ZAP70 expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate Inhibition of human full-length C-terminal His6-tagged ZAP70 expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate	[PMID: 30755337]
Sf21	IC₅₀	261 nM Compound: JTE-952; (S)-8b	Inhibition of recombinant human N-terminal His6-tagged TrkA (440 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate Inhibition of recombinant human N-terminal His6-tagged TrkA (440 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate	[PMID: 30755337]
Sf9	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human N-terminal GST-tagged c-RAF Y340D/Y341D double mutant (306 to 648 residues) expressed in baculovirus infected Sf9 insect cells using MEK1(K97R) as substrate measured after 1 hr Inhibition of human N-terminal GST-tagged c-RAF Y340D/Y341D double mutant (306 to 648 residues) expressed in baculovirus infected Sf9 insect cells using MEK1(K97R) as substrate measured after 1 hr	[PMID: 30755337]
Sf9	IC₅₀	> 1000 nM Compound: JTE-952; (S)-8b	Inhibition of human full-length N-terminal His-tagged SRC expressed in baculovirus infected Sf9 insect cells using Poly-(Glu4:Tyr) as substrate measured after 35 mins Inhibition of human full-length N-terminal His-tagged SRC expressed in baculovirus infected Sf9 insect cells using Poly-(Glu4:Tyr) as substrate measured after 35 mins	[PMID: 30755337]

体内研究
(In Vivo)

JTE-952 (3 mg/kg, p.o. once-daily) treatment reduces the overall progression of the clinical score, including inflammation and bone erosion in mouse model of collagen-induced arthritis (CIA model)^[1].

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

Animal Model:	Mouse model of collagen-induced arthritis (CIA model)^[1].
Dosage:	3 mg/kg.
Administration:	Oral once-daily.
Result:	Reduced the overall progression of the clinical score, including inflammation and bone erosion.

分子量

518.60

Formula

C₃₀H₃₄N₂O₆

CAS 号

1255303-54-8

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

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (192.83 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9283 mL	9.6413 mL	19.2827 mL
5 mM	0.3857 mL	1.9283 mL	3.8565 mL
10 mM	0.1928 mL	0.9641 mL	1.9283 mL

查看完整储备液配制表

* 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 (sealed storage, away from moisture and light)。-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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.95%

选择批次：

Data Sheet (595 KB) SDS (251 KB)

COA (258 KB) HNMR (271 KB) RP-HPLC (262 KB) MS (69 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Ikegashira K, et al. Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952. Bioorg Med Chem Lett. 2019 Apr 1;29(7):873-877. [Content Brief]

JTE-952 相关分类

Inflammation/Immunology

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9283 mL	9.6413 mL	19.2827 mL	48.2067 mL
	5 mM	0.3857 mL	1.9283 mL	3.8565 mL	9.6413 mL
	10 mM	0.1928 mL	0.9641 mL	1.9283 mL	4.8207 mL
	15 mM	0.1286 mL	0.6428 mL	1.2855 mL	3.2138 mL
	20 mM	0.0964 mL	0.4821 mL	0.9641 mL	2.4103 mL
	25 mM	0.0771 mL	0.3857 mL	0.7713 mL	1.9283 mL
	30 mM	0.0643 mL	0.3214 mL	0.6428 mL	1.6069 mL
	40 mM	0.0482 mL	0.2410 mL	0.4821 mL	1.2052 mL
	50 mM	0.0386 mL	0.1928 mL	0.3857 mL	0.9641 mL
	60 mM	0.0321 mL	0.1607 mL	0.3214 mL	0.8034 mL
	80 mM	0.0241 mL	0.1205 mL	0.2410 mL	0.6026 mL
	100 mM	0.0193 mL	0.0964 mL	0.1928 mL	0.4821 mL

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.

Keywords:

JTE-9521255303-54-8JTE952JTE 952c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RInhibitorinhibitorinhibit

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JTE-952

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