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Product details

名称

GW280264X

英文名称

GW280264X

货号

G646226-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC 50 s of 8.0 nM and 11.5 nM, respectively ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells . In Vitro The proliferation of GS-7 cells was significantly reduced upon treatment with GW280264X or ADAM10/17 co-knockdown. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Glioblastoma-initiating cells (GIC) GS-7 cells Concentration: 0.1, 1, and 3 µM Incubation Time: 48 hours Result: Proliferation of GIC is inhibited through inhibition of ADAM10 and ADAM17. In Vivo Pharmacological inhibition of ADAM10 and ADAM17 improves functional recovery after spinal cord injury (SCI). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 miceDosage: 100 µg/kg Administration: I.p. injected; every day for one week starting 4 h post-surgery Result: Showed significantly improved functional recovery compared to the control group. Form:Solid IC50& Target:ADAM17 8 nM (IC 50 ) ADAM10 11.5 nM (IC 50 )

生化机理

GW280264X 是 ADAM10/TACE (ADAM17) 金属蛋白酶混合抑制剂。GW280264X 能有效阻断 TACE（ADAM17）和 ADAM10，其 IC 50 s 分别为 8.0 nM 和 11.5 nM。ADAM10 和 17 可调节胶质母细胞瘤诱导细胞的免疫原性

CAS号

866924-39-2

分子式

C28H41N5O6S

分子量

575.72 g/mol

PubChem编号

91885425

Isomeric SMILES

CCC[C@@H]([C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(=O)OCC1=CC=CC=C1)C(=O)NC2=NC=CS2)N(C=O)O

IIUPAC Name

benzyl N-[(5S)-5-[[(2R,3S)-3-[formyl(hydroxy)amino]-2-(2-methylpropyl)hexanoyl]amino]-6-oxo-6-(1,3-thiazol-2-ylamino)hexyl]carbamate

INCHI

1S/C28H41N5O6S/c1-4-10-24(33(38)19-34)22(17-20(2)3)25(35)31-23(26(36)32-27-29-15-16-40-27)13-8-9-14-30-28(37)39-18-21-11-6-5-7-12-21/h5-7,11-12,15-16,19-20,22-24,38H,4,8-10,13-14,17-18H2,1-3H3,(H,30,37)(H,31,35)(H,29,32,36)/t22-,23+,24+/m1/s1

InChi Key

SKJLITFHSZNZMQ-SGNDLWITSA-N

Smiles

CCCC(C(CC(C)C)C(=O)NC(CCCCNC(=O)OCC1=CC=CC=C1)C(=O)NC2=NC=CS2)N(C=O)O

PubChem CID

91885425

溶解性

DMSO : 125 mg/mL (217.12 mM; ultrasonic and warming and heat to 60°C)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

575.278 Da

单同位素质量Monoisotopic Mass

575.278 Da

拓扑极表面积Topological Polar Surface Area

178.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

782.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

4.100

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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