2. TGF-beta/Smad
  3. TGF-β Receptor
  4. HM-279

HM-279 是一种强效且口服有效的 ALK5 抑制剂，其 IC50 为 4.7 nM。HM-279 与 ALK7 存在交叉反应（IC50 = 6.8 nM），但对其他 TGF-β 受体家族激酶具有中等至良好的选择性，选择性倍数为 4.5 至 693 倍。HM-279 通过 CD8+ T 细胞免疫在体内表现出抗肿瘤活性。HM-279 可用于结肠癌的研究。

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HM-279

HM-279 Chemical Structure

CAS No. : 3039954-64-5

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HM-279 相关抗体

Top Publications Citing Use of Products

查看 TGF-β Receptor 亚型特异性产品:

查看所有亚型
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HM-279 is a potent and orally active ALK5 inhibitor with an IC50 of 4.7 nM. HM-279 shows cross-reactivity with ALK7 (IC50 = 6.8 nM), but HM-279 has fair to good selectivity against other TGF-β receptor family kinases, with 4.5-693-fold selectivity. HM-279 demonstrates antitumor activity in vivo through CD8+ T cell immunity. HM-279 can be used for the research of colon cancer[1].

IC50 & Target[1]

ALK5

4.7 nM (IC50)

ALK7

6.8 nM (IC50)

ALK1

21.0 nM (IC50)

ALK2

64.7 nM (IC50)

BMPR1A

269 nM (IC50)

ALK4

34.6 nM (IC50)

ALK6

999 nM (IC50)

ACVR2A

671 nM (IC50)

ACVR2B

364 nM (IC50)

体外研究
(In Vitro)

HM-279 具有优异的激酶选择性，仅抑制 9 种激酶：AurA、BUB1/BUB3、FLT4、KDR、NuaK1、PDGFRα、PDGFRβ、QIK 和 MST1[1]。
HM-279 对 CT26 细胞的抗增殖活性很弱 (IC50 = 15 μM)[1]。
HM-279 (1.5 h；1-300 nM) 能强烈抑制 A549 细胞中 Smad3 的磷酸化 (IC50 = 21.6 nM)[1]。

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

HM-279 相关抗体:

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 1 nM; 3 nM; 10 nM; 30 nM; 100 nM; 300 nM
Incubation Time: 1.5 h
Result: Completely inhibited the phosphorylation of Smad3 in 300 nM group.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-inf Vss CL MRT0-inf F T1/2
Dog 1 mg/kg i.v. / / / / / / / /
Dog 6.72 mg/kg p.o. / / / / / / / /
Mice 30 mg/kg p.o. / / / / / / / /
Mice 5 mg/kg i.v. 0.5 h 9724 ng/mL 15796 ng·h/mL 0.21 L/kg 0.32 L/h/kg 0.65 h 44 % 0.59 h
Rat 1 mg/kg i.v. / / / / / / / /
Rat 10 mg/kg p.o. / / / / / / / /
体内研究
(In Vivo)

在皮下接种 CT26.WT 细胞的雌性 BALB/cCrSlc 小鼠中，HM-279 (30 mg/kg；口服；用药 5 天/停药 2 天；持续 20 天) 通过调节抗肿瘤免疫而非直接杀伤癌细胞发挥抗肿瘤活性[1]。
HM-279 (30 mg/kg；口服；5 天用药/2 天停药；持续 15 天) 在雌性 BALB/c Slc-nu/nu 小鼠和接受抗 CD8 抗体 (5 mg/kg；腹腔注射；每周两次) 处理的雌性 BALB/cCrSlc 小鼠中均失去抗肿瘤活性，证实了 CD8+ T 细胞参与了 HM-279 引起的抗肿瘤免疫反应[1]。

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

Animal Model: Female BALB/c Slc-nu/nu mice (7 weeks old) were inoculated subcutaneously in the flank with CT26.WT cells (1 × 106 cells) to establish a xenograft model[1].
Dosage: 30 mg/kg
Administration: p.o.; 5 days ON/2 days OFF; for 15 days
Result: Did not have antitumor activity.
Animal Model: Female BALB/cCrSlc mice (7 weeks old) were handled with the anti-CD8 antibody (5 mg/kg; i.p.; twice a week) or isotype control antibody (5 mg/kg; i.p.; twice a week) to establish a CD8-depletion model. Then the mice were inoculated subcutaneously in the flank with CT26.WT cells (1 × 106 cells)[1].
Dosage: 30 mg/kg
Administration: p.o.; 5 days ON/2 days OFF; for 15 days
Result: Did not have antitumor activity in the isotype combination group and the anti-CD8 combination group.
Animal Model: Female BALB/cCrSlc mice (7 weeks old) were inoculated subcutaneously in the flank with CT26.WT cells (1 × 106 cells) to establish a syngeneic model[1].
Dosage: 30 mg/kg; 30 mg/kg plus anti-PD-1 antibody (10 mg/kg; i.p.; BIW)
Administration: p.o.; 5 days ON/2 days OFF; for 20 days
Result: Showed partial antitumor activity with TGI of 60% without body weight loss in orally administration.
When used in combination with anti-PD-1 antibody, the TGI was 89%.
分子量

451.54

Formula

C22H25N7O2S
CAS 号
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.
纯度 & 产品资料
参考文献

HM-279 相关分类

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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:

HM-2793039954-64-5HM279HM 279TGF-β ReceptorTransforming growth factor beta receptorsALK5 inhibitororally activeCD8+ T cell immunityInhibitorinhibitorinhibit

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