LY2157299

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LY2157299 (Galunisertib) 是一种有效、特异性的 TGF-β 受体 I 激酶 ((TGF-βRI)) 抑制剂，IC50 为 56 nM。

LY2157299 (Galunisertib) is a potent, specific inhibitor of TGF-β receptor I kinase ((TGF-βRI) with IC50 of 56 nM; inhibits TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells in a dose-dependent manner, stimulates hematopoiesis from primary MDS bone marrow specimens; ameliorates anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure; displays significant antitumor activity against both Calu6 and MX1 xenografts in mice.Blood Cancer Phase 3 Clinical(In Vitro):Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines.(In Vivo):Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration.

Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines.

Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration.

Galunisertib | LY-2157299 | LY 2157299

TGF-beta/Smad

TGFBR

TβRI

Cancer

Blood cancer

700874-72-2

369.4192

C22H19N5O

>98% (HPLC)

DMSO: ≥ 47 mg/mL

O=C(C1=CC=C2N=CC=C(C3=C(CCC4)N4N=C3C5=NC(C)=CC=C5)C2=C1)N

6-Quinolinecarboxamide, 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-

(-20℃)

With Ice Pack

≥ 2 years