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

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.

For research use only. We do not sell to patients.

HM-279

HM-279 Chemical Structure

CAS No. : 3039954-64-5

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HM-279 Related Antibodies

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

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Description

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)

In Vitro

HM-279 exhibits an excellent kinase selectivity and inhibits only 9 kinases: AurA, BUB1/BUB3, FLT4, KDR, NuaK1, PDGFRα, PDGFRβ, QIK, and MST1[1].
HM-279 has very weak antiproliferative activity against CT26 cells (IC50 = 15 μM). HM-279 (1.5 h; 1-300 nM) strongly inhibits the phosphorylation of Smad3 in A549 cells (IC50 = 21.6 nM)[1].

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

HM-279 Related Antibodies

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.
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. / / / / / / / /
In Vivo

HM-279 (30 mg/kg; p.o.; 5 days ON/2 days OFF; for 20 days) induces antitumor activity through modulation of antitumor immunity rather than direct cytotoxicity to cancer cells in female BALB/cCrSlc mice inoculated subcutaneously with CT26.WT cells[1].
HM-279 (30 mg/kg; p.o.; 5days ON/2days OFF; for 15 days) loses its antitumor activity in both female BALB/c Slc-nu/nu mice and female BALB/cCrSlc mice handled with the anti-CD8 antibody (5 mg/kg; i.p.; twice a week), confirming the involvement of CD8+ T cells in the antitumor immune response elicited by HM-279[1].

MedChemExpress (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%.
Molecular Weight

451.54

Formula

C22H25N7O2S
CAS No.
SMILES

NC(C1=C(C2=CC(C(N(C)C)=O)=CN2)SC(N(CC3CC3)C4=CN(CC#CC)N=C4)=N1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HM-279 Related Classifications

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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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