Talmapimod hydrochloride

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CAS NO:

309915-12-6

SCIO-469 hydrochloride

Talmapimod (SCIO-469) hydrochloride 是p38α选择性的，具有口服活性的，ATP 竞争性的抑制剂，IC₅₀值是 9 nM，约为 p38β 的 10 倍，在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。

生物活性

Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitivep38αinhibitor with anIC₅₀of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity overp38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs^[1]^[2]^[3].

IC₅₀& Target

p38α

9 nM (IC₅₀)

p38β

90 nM (IC₅₀)

体外研究
(In Vitro)

Talmapimod (SCIO-469) hydrochloride (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells^[1].
Talmapimod hydrochloride inhibits LPS-induced TNF-a production in human whole blood^[2].
Talmapimod hydrochloride decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells^[3].

Western Blot Analysis^[1]

Cell Line:	MM.1S, U266, RPMI8226, MM.1R, and RPMI-Dox40 cell lines
Concentration:	100, 200 nM
Incubation Time:	1 hour
Result:	Strongly inhibits phosphorylation of p38 MAPK.

体内研究
(In Vivo)

Talmapimod hydrochloride (10-90 mg/kg; P.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination^[4].

Animal Model:	Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)^[4]
Dosage:	10, 30, 90 mg/kg
Administration:	P.o.; twice daily orally for 14 days
Result:	Dose-dependently reduced tumor growth.

Clinical Trial

分子量

549.46

Formula

C₂₇H₃₁Cl₂FN₄O₃

CAS 号

309915-12-6

中文名称

他匹莫德盐酸盐

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.