>>

>>

抑制剂/激活剂

>>

凋亡与自噬

>>

Crenolanib CP-868596

Crenolanib 是有效和选择性的野生型和突变型 III 类受体酪氨酸激酶抑制剂，抑制 FLT3 和 PDGFRα/β 的 Kd 分别为 0.74 nM，2.1 nM，3.2 nM。

货号：
TK0559
规格：

2mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	670220-88-9
生物活性	Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
分子式	C26H29N5O2
分子量	443.54
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 25 mg/mL (56.36 mM; ultrasonic and warming and heat to 60°C)
体内研究	Crenolanib (10 mg/kg and 20 mg/kg) suppresses non-small-cell lung cancer tumor growth in vivo and induces tumor cell apoptosis, and the dosage of crenolanib applied is well tolerated by recipient mice.
体外研究	Crenolanib has 25-fold more affinity for PDGFRA/B compared with KIT, and is approximately 135-fold more potent than STI571 for inhibiting the PDGFRA D842V mutation. The IC50 for crenolanib for a KIT exon 11 deletion mutant kinase is greater than 1,000 versus 8 nM for STI571. Crenolanib has low nanomolar potency against the V561D + D842V-mutant kinase that is similar to its potency against the isolated D842V mutation. Both STI571 and crenolanib potently inhibit the kinase activity of the fusion oncogene with IC50 values of 1 and 21 nM, respectively, and inhibits PDGFRA activation in this cell line with IC50 values of 93 and 26 nM, respectively. HL60/VCR and K562/ABCB1 cells, overexpressing ABCB1, are 6.9- and 3.6-fold resistant to crenolanib, respectively, in relation to parental HL60 and K562 cells. PSC-833 fully reverses resistance to crenolanib in both HL60/VCR and K562/ABCB1 cells. Crenolanib (1 nM-10 μM) stimulates ABCB1 ATPase activity in a concentration-dependent manner. Crenolanib treatment does not increase the cell surface expression of ABCB1. Crenolanib inhibits [I]-IAAP photocrosslinking of ABCB1 at high concentrations, with 50 % inhibition at 10 μM, but has little effect at lower concentrations, below 1 μM. Crenolanib decreases NSCLC cell viability, induces apoptosis in NSCLC cells, and inhibits cell migration in NSCLC cells.
文献	•Blood. 2018 Jan 25;131(4):426-438. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Glia. 2020 Feb;68(2):345-355. •J Med Chem. 2019 Mar 14;62(5):2428-2446. •Stem Cell Res Ther. 2015 Dec 10;6:243. •Mol Cancer Res. 2021 Oct 11. •Br J Haematol. 2019 Nov;187(4):488-501. •Research Square Preprint. 2021 Nov. •Patent. US20200129476A1 •bioRxiv. 2019 Jul 1.
纯度及产品资料	98%

推荐产品